Indazolesulfonylurea derivative, its use and intermediate for its production

ABSTRACT

The present invention provides an indazolesulfonylurea derivative represented by the general formula:   &lt;IMAGE&gt;    &lt;IMAGE&gt;   [wherein R1 is a hydrogen atom or an alkyl group, etc., R2 and R3 are the same or different and represent a hydrogen atom, a halogen atom, an alkyl group, the formula -COR4 (wherein R4 represents an alkoxy group, etc.), an alkoxy group, a haloalkoxy group or a cyano group, etc., X is an oxygen atom or a sulfur atom, Y is a hydrogen atom or an alkyl group, etc., A and B are the same or different and represent a halogen atom, an alkoxy group or an alkyl group, etc., and Z represents a nitrogen atom or a methine group], as well as a herbicide containing it as an active ingredient and an intermediate for its production. The compound of the present invention exhibits excellent herbicidal effects over a wide range from the preemergence stage to the growing stage of various weeds which are problematic in agricultural fields. Further, it is capable of controlling weeds germinating in paddy fields.

This is a Division of application Ser. No. 08/630,092 filed on Apr. 9,1996, now U.S. Pat. No. 5,670,452, which is a Division of applicationSer. No. 08/373,273 filed on Jan. 30, 1995, now U.S. Pat. No. 5,534,481,which was originally filed as International Application No.PCT/JP94/01016 filed on Jun. 24, 1994.

TECHNICAL FIELD

The present invention relates to a novel indazolesulfonylurea derivative(hereinafter referred to as a compound of the present invention), anintermediate for its production and a herbicide containing it as anactive ingredient.

BACKGROUND ART

Heretofore, many sulfonylurea derivatives such as sulfometuron-methylhave been known as herbicides. Japanese Unexamined Patent PublicationNo. 95091/1992 discloses a herbicide containing an indazolesulfonylureaas an active ingredient. However, the compound of the present inventioni.e. a sulfonylurea derivative having a sulfamoyl group substituted atthe 3-position of an indazole ring, has not been known. Further, theintermediate for its production i.e. an indazolesulfonamide derivative,has also not been known.

It is known that sulfonylurea derivatives have herbicidal activities,but such compounds are not necessarily practically satisfactory, forexample, in that their herbicidal effects are inadequate.

Under these circumstances, the present inventors have conducted variousstudies, and as a result, they have found that the compound of thepresent invention is an excellent herbicide having a high activity andhas finally accomplished the present invention.

DISCLOSURE OF THE INVENTION

Namely, the present invention provides an indazolesulfonylureaderivative represented by the general formula: ##STR2## {wherein R¹ is ahydrogen atom, an alkyl group, a cycloalkyl group, a haloalkyl group, analkoxyalkyl group, a benzyloxyalkyl group, a benzyl group, a phenylgroup, a pyridyl group, a dialkylaminocarbonyl group, an alkoxycarbonylgroup, an alkylsulfonyl group, a phenylsulfonyl group, adialkylaminosulfonyl group, a haloalkylcarbonyl group, an alkylcarbonylgroup, a benzoyl group or an alkenyl group, R² and R³ are the same ordifferent and represent a hydrogen atom, a halogen atom, an alkyl group,a cycloalkyl group, an alkenyl group, an alkoxycarbonylalkenyl group, analkynyl group, a haloalkyl group, an alkoxyalkyl group, analkoxycarbonylalkyl group, an alkylcarbonylalkyl group, acycloalkylcarbonylalkyl group, a cyanoalkyl group, adialkylaminocarbonylalkyl group, a dialkylaminoalkyl group, adialkylaminosulfonylalkyl group, an azidoalkyl group, a benzyl group, aphenyl group, a nitro group, a cyano group, an azide group, an aminogroup, a monoalkylamino group, a dialkylamino group, a benzylaminogroup, an alkylcarbonylamino group which may be substituted by a halogenatom, a benzoylamino group, an alkoxycarbonylamino group, aphenoxycarbonylamino group, an alkylsulfonylamino group wherein theamino group may be substituted by an alkyl group, a phenylsulfonylaminogroup wherein the amino group may be substituted by an alkyl group, analkylideneamino group, a benzylideneamino group, a tetrazolyl groupwhich may be substituted, a group represented by the formula --COR⁴(wherein R⁴ is a hydrogen atom, a hydroxyl group, an alkyl group, acycloalkyl group, a haloalkyl group, an alkenyl group, an alkynyl group,a benzyl group, a phenyl group, an alkoxy group, a haloalkoxy group, analkoxyalkoxy group, an alkenyloxy group, a haloalkenyloxy group, analkynyloxy group, a benzyloxy group or a phenoxy group), a grouprepresented by the formula --C(O)NR⁵ R⁶ (wherein R⁵ and R⁶ are the sameor different and represent a hydrogen atom, an alkyl group, an alkenylgroup, an alkynyl group, a benzyl group, a phenyl group or an alkoxygroup), a group represented by the formula --SR⁷ (wherein R⁷ is ahydrogen atom, an alkyl group or a haloalkyl group), a group representedby the formula --SO₂ NR⁵ R⁶ (wherein R⁵ and R⁶ have the same meanings asdefined above), a group represented by the formula --S(O)_(n) R⁸(wherein n represents an integer of 1 or 2, and R⁸ represents an alkylgroup, an alkenyl group or a haloalkyl group), a group represented bythe formula --OR⁹ wherein R⁹ is a hydrogen atom, an alkyl group, acycloalkylalkyl group, an alkenyl group, an alkynyl group, a benzylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), a haloalkyl group, a haloalkenyl group, a phenylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), an alkoxyalkyl group, an alkoxyalkoxyalkyl group, ahaloalkoxyalkyl group, a benzyloxyalkyl group, a phenoxyalkyl group, analkylthioalkyl group, a dialkylaminoalkyl group, an azidoalkyl group, analkylcarbonyl group, a haloalkylcarbonyl group, a benzoyl group, adialkylaminocarbonyl group, a cyanoalkyl group, an alkylideneaminogroup, a dialkylideneamino group, a benzylideneamino group or analkoxycarbonylalkyl group!, or the formula --C(═NOR¹⁰)R¹¹ (wherein R¹⁰represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynylgroup, a benzyl group, a haloalkyl group or a phenyl group, and R¹¹represents a hydrogen atom, an alkyl group, a benzyl group, a haloalkylgroup or a phenyl group), R² and R³ may together form a ring with analkyl group which may contain a hetero atom, A and B are the same ordifferent and represent an alkyl group, a haloalkyl group, an alkoxygroup, a monoalkylamino group, a dialkylamino group, a halogen atom or ahaloalkoxy group, Z represents a methine group or a nitrogen atom, Xrepresents an oxygen atom or a sulfur atom, and Y represents a hydrogenatom, an alkyl group or an alkoxyalkyl group, as well as itsintermediate represented by an indazolesulfonamide derivativerepresented by the formula I-a! or II-a!: ##STR3## {wherein R¹ is ahydrogen atom, an alkyl group, a cycloalkyl group, a haloalkyl group, analkoxyalkyl group, a benzyloxyalkyl group, a benzyl group, a phenylgroup, a pyridyl group, a dialkylaminocarbonyl group, an alkoxycarbonylgroup, an alkylsulfonyl group, a phenylsulfonyl group, adialkylaminosulfonyl group, a haloalkylcarbonyl group, an alkylcarbonylgroup, a benzoyl group or an alkenyl group, R² and R³ are the same ordifferent and represent a hydrogen atom, a halogen atom, an alkyl group,a cycloalkyl group, an alkenyl group, an alkoxycarbonylalkenyl group, analkynyl group, a haloalkyl group, an alkoxyalkyl group, analkoxycarbonylalkyl group, an alkylcarbonylalkyl group, acycloalkylcarbonylalkyl group, a cyanoalkyl group, adialkylaminocarbonylalkyl group, a dialkylaminoalkyl group, adialkylaminosulfonylalkyl group, an azidoalkyl group, a benzyl group, aphenyl group, a nitro group, a cyano group, an azide group, an aminogroup, a monoalkylamino group, a dialkylamino group, a benzylaminogroup, an alkylcarbonylamino group which may be substituted by a halogenatom, a benzoylamino group, an alkoxycarbonylamino group, aphenoxycarbonylamino group, an alkylsulfonylamino group wherein theamino group may be substituted by an alkyl group, a phenylsulfonylaminogroup wherein the amino group may be substituted by an alkyl group, analkylideneamino group, a benzylideneamino group, a tetrazolyl groupwhich may be substituted, a group represented by the formula --COR⁴(wherein R⁴ is a hydrogen atom, a hydroxyl group, an alkyl group, acycloalkyl group, a haloalkyl group, an alkenyl group, an alkynyl group,a benzyl group, a phenyl group, an alkoxy group, a haloalkoxy group, analkoxyalkoxy group, an alkenyloxy group, a haloalkenyloxy group, analkynyloxy group, a benzyloxy group or a phenoxy group), a grouprepresented by the formula --C(O)NR⁵ R⁶ (wherein R⁵ and R⁶ are the sameor different and represent a hydrogen atom, an alkyl group, an alkenylgroup, an alkynyl group, a benzyl group, a phenyl group or an alkoxygroup), a group represented by the formula --SR⁷ (wherein R⁷ is ahydrogen atom, an alkyl group or a haloalkyl group), a group representedby the formula --SO₂ NR⁵ R⁶ (wherein R⁵ and R⁶ have the same meanings asdefined above), a group represented by the formula --S(O)_(n) R⁸(wherein n represents an integer of 1 or 2, and R⁸ represents an alkylgroup, an alkenyl group or a haloalkyl group), a group represented bythe formula --OR⁹ wherein R⁹ is a hydrogen atom, an alkyl group, acycloalkylalkyl group, an alkenyl group, an alkynyl group, a benzylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), a haloalkyl group, a haloalkenyl group, a phenylgroup (said group may be substituted by a halogen atom, an alkyl groupor an alkoxy group), an alkoxyalkyl group, an alkoxyalkoxyalkyl group, ahaloalkoxyalkyl group, a benzyloxyalkyl group, a phenoxyalkyl group, analkylthioalkyl group, a dialkylaminoalkyl group, an azidoalkyl group, analkylcarbonyl group, a haloalkylcarbonyl group, a benzoyl group, adialkylaminocarbonyl group, a cyanoalkyl group, an alkylideneaminogroup, a dialkylideneamino group, a benzylideneamino group or analkoxycarbonylalkyl group!, or the formula --C(═NOR¹⁰)R¹¹ (wherein R¹⁰represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynylgroup, a benzyl group, a haloalkyl group or a phenyl group, and R¹¹represents a hydrogen atom, an alkyl group, a benzyl group, a haloalkylgroup or a phenyl group), and R² and R³ may form a ring with an alkylgroup which may contain a hetero atom}, and a herbicide containing theindazolesulfonylurea as an active ingredient.

The compound of the present invention includes a tautomer, a geometricalisomer and an optical isomer thereof.

In the present invention, the alkyl group means a straight chain orbranched chain alkyl group having from 1 to 30 carbon atoms andincludes, for example, a methyl group, an ethyl group, a n-propyl group,an isopropyl group, a n-butyl group, an isobutyl group, a sec-butylgroup, a t-butyl group, a n-pentyl group, an isoamyl group, a neopentylgroup, a n-hexyl group, an isohexyl group, a 3,3-dimethylbutyl group, an-heptyl group, a 5-methylhexyl group, a 4-methylhexyl group, a3-methylhexyl group, a 4,4-dimethylpentyl group, a n-octyl group, a6-methylheptyl group, a n-nonyl group, a 7-methyloctyl group, a n-decylgroup, a 8-methylnonyl group, a n-undecyl group, a 9-methyldecyl group,a n-dodecyl group, a 10-methylundecyl group, a n-tridecyl group, a11-methyldodecyl group, a n-tetradecyl group, a 12-methyltridecyl group,a n-pentadecyl group, a 13-methyl-tetradecyl group, a n-hexadecyl group,a n-heptadecyl group, a n-octadecyl group, a n-nonadecyl group, and an-eicosyl group.

The alkoxy group and the alkylsulfonyl group mean an (alkyl)--O-- groupand and (alkyl)--SO₂ -- group, respectively, in which the alkyl moietyhas the above-mentioned meaning.

The halogen atom includes fluorine, chlorine, bromine and iodine atoms.

The alkenyl group means a straight chain or branched chain alkenyl grouphaving from 2 to 20 carbon atoms and includes, for example, a vinylgroup, a propenyl group, an isopropenyl group, a butenyl group, apentenyl group, a hexenyl group, a heptenyl group, an octenyl group, a3-methyl-1-butenyl group, and a 4-methyl-1-pentenyl group.

The alkynyl group means a straight chain or branched chain alkynyl grouphaving from 2 to 20 carbon atoms and includes, for example, an ethynylgroup, a propynyl group, a butynyl group, a pentynyl group, a hexynylgroup, a 3,3-dimethyl-1-butynyl group, a 4-methyl-1-pentynyl group, a3-methyl-1-pentynyl group, a 5-methyl-1-hexynyl group, a4-methyl-1-hexynyl group, a 3-methyl-1-hexynyl group, a heptynyl group,an octynyl group, a nonynyl group, a decynyl group, an undecynyl group,a dodecynyl group, a tridecynyl group, a tetradecynyl group, apentadecynyl group, and a hexadecynyl group.

In the above formula I! or II!, as a group of compounds showingpreferred herbicidal effects, compounds may be mentioned wherein R¹represents a hydrogen atom, a methyl group or an ethyl group, R² and R³are the same or different and represent a hydrogen atom, a halogen atom,an alkoxycarbonyl group, a dialkylaminocarbonyl group, an alkoxy group,a haloalkoxy group, an alkenyloxy group, a cyano group or atrifluoromethyl group, A and B are the same or different and represent amethoxy group, a methyl group or a haloalkoxy group, Z represents amethine group or a nitrogen atom, X represents an oxygen atom, and Yrepresents a hydrogen atom.

Now, typical specific examples of the compound of the present inventionrepresented by the formula I! or II! will be exemplified in Tables 1 and2. The compound numbers will be referred to in the subsequentdescription, and when R¹ represents a hydrogen atom, the compound maytake tautomers represented by the formula I! and II!.

The following symbols in the Tables in the present specificationrepresent the following groups, respectively.

    ______________________________________                                        Bn:      Benzyl group  Pr:    n-Propyl group                                  Pen:     n-Pentyl group                                                                              Bu:    n-Butyl group                                   Me:      Methyl group  Ph:    Phenyl group                                    Et:      Ethyl group                                                          ______________________________________                                    

                                      TABLE 1                                     __________________________________________________________________________     ##STR4##                                                                     Comp.                                                                         No. R.sup.1 R.sup.2    R.sup.3  X  Y    A    B   Z  mp.                       __________________________________________________________________________                                                        (°C.)              I-1 Me      Ph         H        O  H    OMe  OMe CH                           I-2 Me      Bn         H        O  H    OMe  OMe CH                           I-3 Me      SH         H        O  H    OMe  OMe CH                           I-4 Me      SMe        H        O  H    OMe  OMe CH                           I-5 Me      SEt        H        O  H    OMe  OMe CH 189-190                   I-6 Me      SPr        H        O  H    OMe  OMe CH 162-164                   I-7 Me      SO.sub.2 Me                                                                              H        O  H    OMe  DMe CH                           I-8 Me      SO.sub.2 Et                                                                              H        O  H    OMe  OMe CH 157-160                   I-9 Me      SOMe       H        O  H    OMe  OMe CH                           I-10                                                                              Me      SO.sub.2 NHMe                                                                            H        O  H    OMe  OMe CH                           I-11                                                                              Me      SO.sub.2 NHOMe                                                                           H        O  H    OMe  OMe CH                           I-12                                                                              Me      SO.sub.2 NMe.sub.2                                                                       H        O  H    OMe  OMe CH 214-216                   I-13                                                                              Me      SO.sub.2 NHBn                                                                            H        O  H    OMe  OMe CH                           I-14                                                                              Me      SO.sub.2 NHPh                                                                            H        O  H    OMe  OMe CH                           I-15                                                                              Me      SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                           H        O  H    OMe  OMe CH                           I-16                                                                              Me      SO.sub.2 NHCH.sub.2 CCH                                                                  H        O  H    OMe  OMe CH                           I-17                                                                              H       Cl         H        O  H    OMe  OMe CH 191-193                   I-18                                                                              Me      Cl         H        O  H    Me   Me  CH 195-198                   I-19                                                                              Me      Cl         5-Cl     O  H    OMe  OMe CH 210-213                   I-20                                                                              Et      Cl         H        O  H    OMe  OMe CH 187-189                   I-21                                                                              Ph      Cl         H        O  H    OMe  OMe CH                           I-22                                                                              Bn      Cl         H        O  H    OMe  OMe CH                           I-23                                                                              Me      H          H        O  H    OMe  OMe CH 181-183                   I-24                                                                              Me      H          H        O  H    Me   Me  CH                           I-25                                                                              Me      H          H        O  H    OMe  Me  N  172-174                   I-26                                                                              Me      F          H        O  H    OMe  OMe CH 205-209                   I-27                                                                              Me      Br         H        O  H    OMe  OMe CH 276-279                   I-28                                                                              Me      Me         H        O  H    OMe  OMe CH 178-180                   I-29                                                                              Me      CN         H        O  H    OMe  OMe CH 267-269                   I-30                                                                              Me      CF.sub.3   H        O  H    OMe  OMe CH                           I-31                                                                              Me      Cl         H        O  H    OMe  Me  CH 243-245                   I-32                                                                              Me      Cl         H        O  H    OMe  Me  N  266-267                   I-33                                                                              Me      F          H        O  H    Me   Me  CH 195-197                   I-34                                                                              Me      F          H        O  H    OMe  Me  N  197-200                   I-35                                                                              Me      F          H        O  H    OMe  Me  CH 180-185                   I-36                                                                              Me      H          5-Cl     O  H    OMe  OMe CH                           I-37                                                                              Me      H          5-Cl     O  H    Me   Me  CH                           I-38                                                                              Me      H          5-Cl     O  H    OMe  Me  N                            I-39                                                                              Me      H          6-Cl     O  H    OMe  OMe CH                           I-40                                                                              Me      H          6-Cl     O  H    Me   Me  CH                           I-41                                                                              Me      H          6-Cl     O  H    OMe  Me  N                            I-42                                                                              Me      H          7-Cl     O  H    OMe  OMe CH                           I-43                                                                              Me      H          7-Cl     O  H    OMe  Me  N                            I-44                                                                              Me      Cl         H        S  H    OMe  OMe CH                           I-45                                                                              Me      Cl         H        O  Me   OMe  OMe CH                           I-46                                                                              Me      COH        H        O  H    OMe  OMe CH                           I-47                                                                              Me      COMe       H        O  H    OMe  OMe CH                           I-48                                                                              Me      COEt       H        O  H    OMe  OMe CH                           I-49                                                                              Me      COPh       H        O  H    OMe  OMe CH                           I-50                                                                              Me      COCH.sub.2 CHCH.sub.2                                                                    H        O  H    OMe  OMe CH                           I-51                                                                              Me      COCH.sub.2 CCH                                                                           H        O  H    OMe  OMe CH                           I-52                                                                              Me      COBn       H        O  H    OMe  OMe CH                           I-53                                                                              Me      NO.sub.2   H        O  H    OMe  OMe CH 219-220                   I-54                                                                              Me      NH.sub.2   H        O  H    OMe  OMe CH                           I-55                                                                              Me      NHMe       H        O  H    OMe  OMe CH                           I-56                                                                              Me      NMe.sub.2  H        O  H    OMe  OMe CH                           I-57                                                                              Me      NHCOMe     H        O  H    OMe  OMe CH                           I-58                                                                              Me      NHCOPh     H        O  H    OMe  OMe CH                           I-59                                                                              Me      NHCOCH.sub.2 Cl                                                                          H        O  H    OMe  OMe CH                           I-60                                                                              Me      NHSO.sub.2 CH.sub.3                                                                      H        O  H    OMe  OMe CH                           I-61                                                                              Me      NHSO.sub.2 Ph                                                                            H        O  H    OMe  OMe CH                           I-62                                                                              Me      CO.sub.2 H H        O  H    OMe  OMe CH                           I-63                                                                              Me      CO.sub.2 Me                                                                              H        O  H    OMe  OMe CH 187-190                   I-64                                                                              Me      CO.sub.2 Et                                                                              H        O  H    OMe  OMe CH 192-195                   I-65                                                                              Me      CO.sub.2 Pr                                                                              H        O  H    OMe  OMe CH 195-197                   I-66                                                                              Me      CO.sub.2 Pr-i                                                                            H        O  H    OMe  OMe CH 168-169                   I-67                                                                              Me      CO.sub.2 Bu                                                                              H        O  H    OMe  OMe CH 169-172                   I-68                                                                              Me      CO.sub.2 Pen                                                                             H        O  H    OMe  OMe CH                           I-69                                                                              Me      CO.sub.2 Bn                                                                              H        O  H    OMe  OMe CH                           I-70                                                                              Me      CO.sub.2 Ph                                                                              H        O  H    OMe  OMe CH                           I-71                                                                              Me      CO.sub.2 CH.sub.2 CH.sub.2 F                                                             H        O  H    OMe  OMe CH                           I-72                                                                              Me      CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    OMe  OMe CH                           I-73                                                                              Me      CO.sub.2 CH.sub.2 CCH                                                                    H        O  H    OMe  OMe CH                           I-74                                                                              Me      CO.sub.2 Me                                                                              H        O  H    OCHF.sub.2                                                                         OCHF.sub.2                                                                        CH                           I-75                                                                              Me      CO.sub.2 Et                                                                              H        O  H    OCHF.sub.2                                                                         OCHF.sub.2                                                                        CH                           I-76                                                                              Me      CO.sub.2 Me                                                                              H        O  H    OMe  Cl  CH                           I-77                                                                              Me      CO.sub.2 Me                                                                              H        O  H    OMe  Me  CH                           I-78                                                                              Me      CO.sub.2 Me                                                                              H        O  H    OMe  Me  N                            I-79                                                                              Me      CO.sub.2 Et                                                                              H        O  H    OMe  Me  N  193-196                   I-80                                                                              Me      CO.sub.2 Me                                                                              H        O  H    OMe  OCHF.sub.2                                                                        CH                           I-81                                                                              Me      CO.sub.2 Me                                                                              5-F      O  H    OMe  OMe CH                           I-82                                                                              Et      CO.sub.2 Me                                                                              H        O  H    OMe  OMe CH 182-183                   I-83                                                                              Bu      CO.sub.2 Me                                                                              H        O  H    OMe  OMe CH                           I-84                                                                              Bn      CO.sub.2 Me                                                                              H        O  H    OMe  OMe CH                           I-85                                                                              Ph      CO.sub.2 Me                                                                              H        O  H    OMe  OMe CH                           I-86                                                                              H       CO.sub.2 Et                                                                              H        O  H    OMe  OMe CH                           I-87                                                                              Me      CO.sub.2 Me                                                                              H        S  H    OMe  OMe CH                           I-88                                                                              Me      CO.sub.2 Et                                                                              H        S  H    OMe  OMe CH                           I-89                                                                              Me      CO.sub.2 Me                                                                              H        O  Me   OMe  OMe CH                           I-90                                                                              Me      DH         H        O  H    OMe  OMe CH                           I-91                                                                              Me      OMe        H        O  H    OMe  OMe CH 265-267                   I-92                                                                              Me      OEt        H        O  H    OMe  OMe CH 162-164                   I-93                                                                              Me      OPr        H        O  H    OMe  OMe CH 134-136                   I-94                                                                              Me      OPr-i      H        O  H    OMe  OMe CH 168-171                   I-95                                                                              Me      OBu        H        O  H    OMe  OMe CH 198-200                   I-96                                                                              Me      OBn        H        O  H    OMe  OMe CH                           I-97                                                                              Me      OBn(4-Cl)  H        O  H    OMe  OMe CH                           I-98                                                                              Me      OBn(3-OMe) H        O  H    OMe  OMe CH                           I-99                                                                              Me      OBn(2-Me)  H        O  H    OMe  OMe CH                           I-100                                                                             Me      OPh        H        O  H    OMe  OMe CH                           I-101                                                                             Me      OPh(4-Cl)  H        O  H    OMe  OMe CH                           I-102                                                                             Me      OPh(3-OMe) H        O  H    OMe  OMe CH                           I-103                                                                             Me      OPh(2-Me)  H        O  H    OMe  OMe CH                           I-104                                                                             Me      OCH.sub.2 CHCH.sub.2                                                                     H        O  H    OMe  OMe CH                           I-105                                                                             Me      OCH.sub.2 CCH                                                                            H        O  H    OMe  OMe CH                           I-106                                                                             Me      OCH.sub.2 CF.sub.3                                                                       H        O  H    OMe  OMe CH                           I-107                                                                             Me      OCH.sub.2 CH.sub.2 OMe                                                                   H        O  H    OMe  OMe CH                           I-108                                                                             Me      OCH.sub.2 CH.sub.2 OPh                                                                   H        O  H    OMe  OMe CH                           I-109                                                                             Me      OCOMe      H        O  H    OMe  OMe CH                           I-110                                                                             Me      OMe        H        O  H    OMe  Me  CH                           I-111                                                                             Me      OMe        H        O  H    OMe  Me  N  269-270                   I-112                                                                             Me      OMe        H        O  H    Me   Me  CH 267-268                   I-113                                                                             Me      OEt        H        O  H    OMe  Cl  CH 160-165                   I-114                                                                             Me      OEt        H        O  H    OMe  Me  CH 169-170                   I-115                                                                             Me      OEt        H        O  H    Me   Me  CH                           I-116                                                                             Me      CONH.sub.2 H        O  H    OMe  OMe CH                           I-117                                                                             Me      CONHMe     H        O  H    OMe  OMe CH                           I-118                                                                             Me      CONHEt     H        O  H    OMe  OMe CH                           I-119                                                                             Me      CONHPr     H        O  H    OMe  OMe CH                           I-120                                                                             Me      CONMe.sub.2                                                                              H        O  H    OMe  OMe CH 205-207                   I-121                                                                             Me      CONEt.sub.2                                                                              H        O  H    OMe  OMe CH                           I-122                                                                             Me      CONHBn     H        O  H    OMe  OMe CH                           I-123                                                                             Me      CONHPh     H        O  H    OMe  OMe CH                           I-124                                                                             Me      CONHCH.sub.2 CHCH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-125                                                                             Me      CONHCH.sub.2 CCH                                                                         H        O  H    OMe  OMe CH                           I-126                                                                             Me      CONHOMe    H        O  H    OMe  OMe CH                           I-127                                                                             Me      H          5-F      O  H    OMe  OMe CH                           I-128                                                                             Me      H          5-F      O  H    Me   Me  CH                           I-129                                                                             Me      H          5-F      O  H    OMe  Me  CH                           I-130                                                                             Me      H          5-F      O  H    OMe  Me  N                            I-131                                                                             H       COOMe      H        O  H    OMe  OMe CH 179-180                   I-132                                                                             H       COOMe      H        O  H    OMe  Cl  CH 193-194                   I-133                                                                             H       Cl         H        O  H    OMe  Cl  CH 178-181                   I-134                                                                             Me      Cl         H        O  H    OMe  OMe CH 265-267                   I-135                                                                             Me      SO.sub.2 NH.sub.2                                                                        H        O  H    OMe  OMe CH                           I-136                                                                             H       Br         H        O  H    OMe  OMe CH 190-193                   I-137                                                                             Me      H          5-OMe    O  H    OMe  OMe CH                           I-138                                                                             Me      H          5-OEt    O  H    OMe  OMe CH                           I-139                                                                             Me      H          5-OPr    O  H    OMe  OMe CH                           I-140                                                                             Me      OCH(CF.sub.3)Me                                                                          H        O  H    OMe  OMe CH                           I-141                                                                             Me      OCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    OMe  OMe CH                           I-142                                                                             Me      OCH.sub.2 CH.sub.2 F                                                                     H        O  H    OMe  OMe CH                           I-143                                                                             Me      OCH.sub.2 CH.sub.2 OEt                                                                   H        O  H    OMe  OMe CH                           I-144                                                                             Me      OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O  H    OMe  OMe CH                           I-145                                                                             Me      OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  OMe CH                           I-146                                                                             Me      OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  OMe CH                           I-147                                                                             Me      OCH.sub.2 COOEt                                                                          H        O  H    OMe  OMe CH                           I-148                                                                             Me      OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O  H    OMe  OMe CH                           I-149                                                                             Me      SBu        H        O  H    OMe  OM& CH 165-168                   I-150                                                                             Me      SPr-i      H        O  H    OMe  OMe CH 178-180                   I-151                                                                             Me      SO.sub.2 Pr                                                                              H        O  H    OMe  OMe CH 163-167                   I-152                                                                             Me      SO.sub.2 Bu                                                                              H        O  H    OMe  OMe CH 187-189                   I-153                                                                             Me      SO.sub.2 Pr-i                                                                            H        O  H    OMe  OMe CH 279-281                   I-154                                                                             Me      NHBn       H        O  H    OMe  OMe CH                           I-155                                                                             Me      NEt.sub.2  H        O  H    OMe  OMe CH                           I-156                                                                             Me      OMe        5-Cl     O  H    OMe  OMe CH                           I-157                                                                             Me      Br         H        O  H    OMe  Me  CH 276-279                   I-158                                                                             Et      Cl         H        O  H    OMe  Me  CH 182-184                   I-159                                                                             Ph      Cl         H        O  H    OMe  Me  CH                           I-160                                                                             Me      OPr        H        O  H    OMe  Me  CH 178-180                   I-161                                                                             Me      OBu        H        O  H    OMe  Me  CH 174-176                   I-162                                                                             Me      OPr-i      H        O  H    OMe  Me  CH 184-186                   I-163                                                                             Me      H          5-OMe    O  H    OMe  Me  CH                           I-164                                                                             Me      H          5-OEt    O  H    OMe  Me  CH                           I-165                                                                             Me      H          5-OPr    O  H    OMe  Me  CH                           I-166                                                                             Me      OCH.sub.2 CF.sub.3                                                                       H        O  H    OMe  Me  CH                           I-167                                                                             Me      OCH(CF.sub.3)Me                                                                          H        O  H    OMe  Me  CH                           I-168                                                                             Me      OCH.sub.2 CH.sub.2 OMe                                                                   H        O  H    OMe  Me  CH                           I-169                                                                             Me      OCH.sub.2 CH.sub.2 OEt                                                                   H        O  H    OMe  Me  CH                           I-170                                                                             Me      OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O  H    OMe  Me  CH                           I-171                                                                             Me      OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  Me  CH                           I-172                                                                             Me      OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  Me  CH                           I-173                                                                             Me      OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O  H    OMe  Me  CH                           I-174                                                                             Me      SPr        H        O  H    OMe  Me  CH 155-156                   I-175                                                                             Me      CO.sub.2 Pr                                                                              H        O  H    OMe  Me  CH 185-186                   I-176                                                                             Me      CO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  CH 158-160                   I-177                                                                             Me      CO.sub.2 Bu                                                                              H        O  H    OMe  Me  CH 174-175                   I-178                                                                             Me      NO.sub.2   H        O  H    OMe  Me  CH 212-214                   I-179                                                                             Me      CN         H        O  H    OMe  Me  CH 180-181                   I-180                                                                             Me      Br         H        O  H    OMe  Me  N  166-169                   I-181                                                                             Et      Cl         H        O  H    OMe  Me  N  141-142                   I-182                                                                             Me      OPr        H        O  H    OMe  Me  N  210-213                   I-183                                                                             Me      OBu        H        O  H    OMe  Me  N  184-186                   I-184                                                                             Me      OPr-i      H        O  H    OMe  Me  N  157-159                   I-185                                                                             Me      H          5-OMe    O  H    OMe  Me  N                            I-186                                                                             Me      H          5-OEt    O  H    OMe  Me  N                            I-187                                                                             Me      H          5-OPr    O  H    dMe  Me  N                            I-188                                                                             Me      OCH.sub.2 CF.sub.3                                                                       H        O  H    OMe  Me  N                            I-189                                                                             Me      OCH.sub.2 CH.sub.2 OEt                                                                   H        o  H    OMe  Me  N                            I-190                                                                             Me      OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O  H    OMe  Me  N                            I-191                                                                             Me      OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  Me  N                            I-192                                                                             Me      OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  Me  N                            I-193                                                                             Me      OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O  H    OMe  Me  N                            I-194                                                                             Me      SEt        H        O  H    OMe  Me  N  223-224                   I-195                                                                             Me      SPr        H        O  H    OMe  Me  N                            I-196                                                                             Me      NMe.sub.2  H        O  H    OMe  Me  N                            I-197                                                                             Me      CO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  N                            I-198                                                                             Me      CO.sub.2 Bu                                                                              H        O  H    OMe  Me  N  177-178                   I-199                                                                             Me      CN         H        O  H    OMe  Me  N  255-258                   I-200                                                                             Me      OMe        5-Cl     O  H    OMe  Me  N                            I-201                                                                             Me      Cl         H        O  H    Cl   OMe CH                           I-202                                                                             Et      Cl         H        O  H    Cl   OMe CH                           I-203                                                                             Ph      Cl         H        O  H    Cl   OMe CH                           I-204                                                                             Me      OMe        H        O  H    Cl   OMe CH 268-269                   I-205                                                                             Me      OPr        H        O  H    Cl   OMe CH 168-169                   I-206                                                                             Me      OBu        H        O  H    Cl   OMe CH 171-173                   I-207                                                                             Me      H          5-OMe    O  H    Cl   OMe CH                           I-208                                                                             Me      OCH.sub.2 CF.sub.3                                                                       H        O  H    Cl   OMe CH                           I-209                                                                             Me      SPr        H        O  H    Cl   OMe CH 143-145                   I-210                                                                             Me      SBu        H        O  H    Cl   OMe CH                           I-211                                                                             Me      SPr-i      H        O  H    Cl   OMe CH 228-230                   I-212                                                                             Me      SO.sub.2 Pr-i                                                                            H        O  H    Cl   OMe CH 143-145                   I-213                                                                             Me      NHBn       H        O  H    Cl   OMe CH                           I-214                                                                             Me      NMe.sub.2  H        O  H    Cl   OMe CH                           I-215                                                                             Et      Cl         H        O  H    Me   Me  CH                           I-216                                                                             Me      OPr        H        O  H    Me   Me  CH 149-150                   I-217                                                                             Me      OBu        H        O  H    Me   Me  CH 146-149                   I-218                                                                             Me      OPr-i      H        O  H    Me   Me  CH 174-176                   I-219                                                                             Me      NMe.sub.2  H        O  H    Me   Me  CH                           I-220                                                                             Me      OMe        H        O  H    OMe  OMe N                            I-221                                                                             Me      H          5-OEt    O  H    OMe  OMe N                            I-222                                                                             Me      H          5-OPr    O  H    OMe  OMe N                            I-223                                                                             Me      OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  OMe N                            I-224                                                                             Me      OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  OMe N                            I-225                                                                             Me      NHMe       H        O  H    OMe  Me  CH                           I-226                                                                             Me      NHMe       H        O  H    OMe  Me  N                            I-227                                                                             Me      OMe        H        O  H    OMe  Me  CH                           I-228                                                                             Me      OMe        5-OMe    O  H    OMe  Me  CH                           I-229                                                                             Me      OCHF.sub.2 H        O  H    OMe  OMe CH 198-200                   I-230                                                                             Me      OCHF.sub.2 H        O  H    Me   OMe CH 177-179                   I-231                                                                             Me      OCHF.sub.2 H        O  H    Me   OMe N  165-167                   I-232                                                                             Me      OCH.sub.2 CHF.sub.2                                                                      H        O  H    OMe  OMe CH                           I-233                                                                             Me      OCH.sub.2 CHF.sub.2                                                                      H        O  H    Me   OMe CH                           I-234                                                                             Me      OCH.sub.2 CHF.sub.2                                                                      H        O  H    Me   OMe N                            I-235                                                                             Me      OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O  H    OMe  OMe CH                           I-236                                                                             Me      OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O  H    Me   OMe CH                           I-237                                                                             Me      OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O  H    Me   OMe N                            I-238                                                                             Me      OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O  H    OMe  OMe CH                           I-239                                                                             Me      OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O  H    Me   OMe CH                           I-240                                                                             Me      OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O  H    Me   OMe N                            I-241                                                                             Me      OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O  H    OMe  OMe CH                           I-242                                                                             Me      OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O  H    Me   OMe CH                           I-243                                                                             Me      OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O  H    Me   OMe N                            I-244                                                                             Me      OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O  H    OMe  OMe CH                           I-245                                                                             Me      OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O  H    Me   OMe CH                           I-246                                                                             Me      OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O  H    Me   OMe N                            I-247                                                                             Me      OCH.sub.2 CHCl.sub.2                                                                     H        O  H    OMe  OMe CH                           I-248                                                                             Me      OCH.sub.2 CHCl.sub.2                                                                     H        O  H    Me   OMe CH                           I-249                                                                             Me      OCH.sub.2 CHCl.sub.2                                                                     H        O  H    Me   OMe N                            I-250                                                                             Me      OCF.sub.2 CH.sub.2 Cl                                                                    H        O  H    OMe  OMe CH                           I-251                                                                             Me      OCF.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe CH                           I-252                                                                             Me      OCF.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe N                            I-253                                                                             Me      OCF.sub.2 CHFCl                                                                          H        O  H    OMe  OMe CH                           I-254                                                                             Me      OCF.sub.2 CHFCl                                                                          H        O  H    Me   OMe CH                           I-255                                                                             Me      OCF.sub.2 CHFCl                                                                          H        O  H    Me   OMe N                            I-256                                                                             Me      OCF.sub.3  H        O  H    OMe  OMe CH                           I-257                                                                             Me      OCF.sub.3  H        O  H    Me   OMe CH                           I-258                                                                             Me      OCF.sub.3  H        O  H    Me   OMe N                            I-259                                                                             Me      OCH.sub.2 CHCHCl                                                                         H        O  H    OMe  OMe CH                           I-260                                                                             Me      OCH.sub.2 CHCHCl                                                                         H        O  H    Me   OMe CH                           I-261                                                                             Me      OCH.sub.2 CHCHCl                                                                         H        O  H    Me   OMe N                            I-262                                                                             Me      OCH.sub.2 CHCCl.sub.2                                                                    H        O  H    OMe  OMe CH                           I-263                                                                             Me      OCH.sub.2 CHCCl.sub.2                                                                    H        O  H    Me   OMe CH                           I-264                                                                             Me      OCH.sub.2 CHCCl.sub.2                                                                    H        O  H    Me   OMe N                            I-265                                                                             Me      OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-266                                                                             Me      OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O  H    Me   OMe CH                           I-267                                                                             Me      OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O  H    Me   OMe N                            I-268                                                                             Me      OCH.sub.2 C(Me)CH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-269                                                                             Me      OCH.sub.2 C(Me)CH.sub.2                                                                  H        O  H    Me   OMe CH                           I-270                                                                             Me      OCH.sub.2 C(Me)CH.sub.2                                                                  H        O  H    Me   OMe N                            I-271                                                                             Me      OCH.sub.2 CHCHMe                                                                         H        O  H    OMe  OMe CH                           I-272                                                                             Me      OCH.sub.2 CHCHMe                                                                         H        O  H    Me   OMe CH                           I-273                                                                             Me      OCH.sub.2 CHCHMe                                                                         H        O  H    Me   OMe N                            I-274                                                                             Me      OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O  H    OMe  OMe CH                           I-275                                                                             Me      OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O  H    Me   OMe CH                           I-276                                                                             Me      OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O  H    Me   OMe N                            I-277                                                                             Me      OCH.sub.2 OMe                                                                            H        O  H    OMe  OMe CH                           I-278                                                                             Me      OCH.sub.2 OMe                                                                            H        O  H    Me   OMe CH                           I-279                                                                             Me      OCH.sub.2 OMe                                                                            H        O  H    Me   OMe N                            I-280                                                                             Me      OCH.sub.2 OEt                                                                            H        O  H    OMe  OMe CH                           I-281                                                                             Me      OCH.sub.2 OEt                                                                            H        O  H    Me   OMe CH                           I-282                                                                             Me      OCH.sub.2 OEt                                                                            H        O  H    Me   OMe N                            I-283                                                                             Me      OCH.sub.2 OBn                                                                            H        O  H    OMe  OMe CH                           I-284                                                                             Me      OCH.sub.2 OBn                                                                            H        O  H    Me   OMe CH                           I-285                                                                             Me      OCH.sub.2 OBn                                                                            H        O  H    Me   OMe N                            I-286                                                                             Me      OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O  H    OMe  OMe CH                           I-287                                                                             Me      OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O  H    Me   OMe CH                           I-288                                                                             Me      OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O  H    Me   OMe N                            I-289                                                                             Me      OCH.sub.2 OBu-t                                                                          H        O  H    OMe  OMe CH                           I-290                                                                             Me      OCH.sub.2 OBu-t                                                                          H        O  H    Me   OMe CH                           I-291                                                                             Me      OCH.sub.2 OBu-t                                                                          H        O  H    Me   OMe N                            I-292                                                                             Me      OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O  H    OMe  OMe CH                           I-293                                                                             Me      OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O  H    Me   OMe CH                           I-294                                                                             Me      OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O  H    Me   OMe N                            I-295                                                                             Me      OCH.sub.2 CN                                                                             H        O  H    OMe  OMe CH                           I-296                                                                             Me      OCH.sub.2 CN                                                                             H        O  H    Me   OMe CH                           I-297                                                                             Me      OCH.sub.2 CN                                                                             H        O  H    Me   OMe N                            I-298                                                                             Me      OCH.sub.2 COOMe                                                                          H        O  H    OMe  OMe CH                           I-299                                                                             Me      OCH.sub.2 COOMe                                                                          H        O  H    Me   OMe CH                           I-300                                                                             Me      OCH.sub.2 COOMe                                                                          H        O  H    Me   OMe N                            I-301                                                                             Me      OCH.sub.2 COOPr                                                                          H        O  H    OMe  OMe CH                           I-302                                                                             Me      OCH.sub.2 COOPr                                                                          H        O  H    Me   OMe CH                           I-303                                                                             Me      OCH.sub.2 COOPr                                                                          H        O  H    Me   OMe N                            I-304                                                                             Me      OCH.sub.2 COOPr-i                                                                        H        O  H    OMe  OMe CH                           I-305                                                                             Me      OCH.sub.2 COOPr-i                                                                        H        O  H    Me   OMe CH                           I-306                                                                             Me      OCH.sub.2 COOPr-i                                                                        H        O  H    Me   OMe N                            I-307                                                                             Me      OCH.sub.2 SMe                                                                            H        O  H    OMe  OMe CH                           I-308                                                                             Me      OCH.sub.2 SMe                                                                            H        O  H    Me   OMe CH                           I-309                                                                             Me      OCH.sub.2 SMe                                                                            H        O  H    Me   OMe N                            I-310                                                                             Me      OCH.sub.2 CH.sub.2 SMe                                                                   H        O  H    OMe  OMe CH                           I-311                                                                             Me      OCH.sub.2 CH.sub.2 SMe                                                                   H        O  H    Me   OMe CH                           I-312                                                                             Me      OCH.sub.2 CH.sub.2 SMe                                                                   H        O  H    Me   OMe N                            I-313                                                                             Me      SCF.sub.3  H        O  H    OMe  OMe CH                           I-314                                                                             Me      SCF.sub.3  H        O  H    Me   OMe CH                           I-315                                                                             Me      SCF.sub.3  H        O  H    Me   OMe N                            I-316                                                                             Me      SCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    OMe  OMe CH                           I-317                                                                             Me      SCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe CH                           I-318                                                                             Me      SCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe N                            I-319                                                                             Me      SCH.sub.2 CH.sub.2 F                                                                     H        O  H    OMe  OMe CH                           I-320                                                                             Me      SCH.sub.2 CH.sub.2 F                                                                     H        O  H    Me   OMe CH                           I-321                                                                             Me      SCH.sub.2 CH.sub.2 F                                                                     H        O  H    Me   OMe N                            I-322                                                                             Me      SOEt       H        O  H    OMe  OMe CH 185-187                   I-323                                                                             Me      SOEt       H        O  H    Me   OMe CH                           I-324                                                                             Me      SOEt       H        O  H    Me   OMe N  136-137 (decomposed)      I-325                                                                             Me      SO.sub.2 NHOEt                                                                           H        O  H    OMe  OMe CH                           I-326                                                                             Me      SO.sub.2 NHOEt                                                                           H        O  H    Me   OMe CH                           I-327                                                                             Me      SO.sub.2 NHOEt                                                                           H        O  H    Me   OMe N                            I-328                                                                             Me      SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    OMe  OMe CH                           I-329                                                                             Me      SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    Me   OMe CH                           I-330                                                                             Me      SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    Me   OMe N                            I-331                                                                             Me      SO.sub.2 NEt.sub.2                                                                       H        O  H    OMe  OMe CH                           I-332                                                                             Me      SO.sub.2 NEt.sub.2                                                                       H        O  H    Me   OMe CH                           I-333                                                                             Me      SO.sub.2 NEt.sub.2                                                                       H        O  H    Me   OMe N                            I-334                                                                             Me      Et         H        O  H    OMe  OMe CH 174-176                   I-335                                                                             Me      Et         H        O  H    Me   OMe CH                           I-336                                                                             Me      Et         H        O  H    Me   OMe N                            I-337                                                                             Me      Pr         H        O  H    OMe  OMe CH 168-171                   I-338                                                                             Me      Pr         H        O  H    Me   OMe CH                           I-339                                                                             Me      Pr         H        O  H    Me   OMe N                            I-340                                                                             Me      Pr-i       H        O  H    OMe  OMe CH                           I-341                                                                             Me      Pr-i       H        O  H    Me   OMe CH                           I-342                                                                             Me      Pr-i       H        O  H    Me   OMe N                            I-343                                                                             Me      Bu         H        O  H    OMe  OMe CH                           I-344                                                                             Me      Bu         H        O  H    Me   OMe CH                           I-345                                                                             Me      Bu         H        O  H    Me   OMe N                            I-346                                                                             Me      Bu-t       H        O  H    OMe  OMe CH                           I-347                                                                             Me      Bu-t       H        O  H    Me   OMe CH                           I-348                                                                             Me      Bu-t       H        O  H    Me   OMe N                            I-349                                                                             Me      CH.sub.2 Cl                                                                              H        O  H    OMe  OMe CH                           I-350                                                                             Me      CH.sub.2 Cl                                                                              H        O  H    Me   OMe CH                           I-351                                                                             Me      CH.sub.2 Cl                                                                              H        O  H    Me   OMe N                            I-352                                                                             Me      CH.sub.2 F H        O  H    OMe  OMe CH                           I-353                                                                             Me      CH.sub.2 F H        O  H    Me   OMe CH                           I-354                                                                             Me      CH.sub.2 F H        O  H    Me   OMe N                            I-355                                                                             Me      CH.sub.2 OMe                                                                             H        O  H    OMe  OMe CH                           I-356                                                                             Me      CH.sub.2 OMe                                                                             H        O  H    Me   OMe CH                           I-357                                                                             Me      CH.sub.2 OMe                                                                             H        O  H    Me   OMe N                            I-358                                                                             Me      CH.sub.2 CF.sub.3                                                                        H        O  H    OMe  OMe CH                           I-359                                                                             Me      CH.sub.2 CF.sub.3                                                                        H        O  H    Me   OMe CH                           I-360                                                                             Me      CH.sub.2 CF.sub.3                                                                        H        O  H    Me   OMe N                            I-361                                                                             Me                                                                                     ##STR5##  H        O  H    OMe  OMe CH                           I-362                                                                             Me                                                                                     ##STR6##  H        O  H    Me   OMe CH                           I-363                                                                             Me                                                                                     ##STR7##  H        O  H    Me   OMe N                            I-364                                                                             Me      CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O  H    OMe  OMe CH                           I-365                                                                             Me      CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O  H    Me   OMe CH                           I-366                                                                             Me      CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O  H    Me   OMe N                            I-367                                                                             Me      CH.sub.2 CHCH.sub.2                                                                      H        O  H    OMe  OMe CH                           I-368                                                                             Me      CH.sub.2 CHCH.sub.2                                                                      H        O  H    Me   OMe CH                           I-369                                                                             Me      CH.sub.2 CHCH.sub.2                                                                      H        O  H    Me   OMe N                            I-370                                                                             Me      CH.sub.2 CCH                                                                             H        O  H    OMe  OMe CH                           I-371                                                                             Me      CH.sub.2 CCH                                                                             H        O  H    Me   OMe CH                           I-372                                                                             Me      CH.sub.2 CCH                                                                             H        O  H    Me   OMe N                            I-373                                                                             Me      CH.sub.2 COOMe                                                                           H        O  H    OMe  OMe CH                           I-374                                                                             Me      CH.sub.2 COOMe                                                                           H        O  H    Me   OMe CH                           I-375                                                                             Me      CH.sub.2 COOMe                                                                           H        O  H    Me   OMe N                            I-376                                                                             Me      CH.sub.2 COOEt                                                                           H        O  H    OMe  OMe CH                           I-377                                                                             Me      CH.sub.2 COOEt                                                                           H        O  H    Me   OMe CH                           I-378                                                                             Me      CH.sub.2 COOEt                                                                           H        O  H    Me   OMe N                            I-379                                                                             Me      CH.sub.2 CN                                                                              H        O  H    OMe  OMe CH                           I-380                                                                             Me      CH.sub.2 CN                                                                              H        O  H    Me   OMe CH                           I-381                                                                             Me      CH.sub.2 CN                                                                              H        O  H    Me   OMe N                            I-382                                                                             Me      CH.sub.2 CONMe.sub.2                                                                     H        O  H    OMe  OMe CH                           I-383                                                                             Me      CH.sub.2 CONMe.sub.2                                                                     H        O  H    Me   OMe CH                           I-384                                                                             Me      CH.sub.2 CONMe.sub.2                                                                     H        O  H    Me   OMe N                            I-385                                                                             Me      CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O  H    OMe  OMe CH                           I-386                                                                             Me      CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O  H    Me   OMe CH                           I-387                                                                             Me      CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O  H    Me   OMe N                            I-388                                                                             Me      CH.sub.2 NMe.sub.2                                                                       H        O  H    OMe  OMe CH                           I-389                                                                             Me      CH.sub.2 NMe.sub.2                                                                       H        O  H    Me   OMe CH                           I-390                                                                             Me      CH.sub.2 NMe.sub.2                                                                       H        O  H    Me   OMe N                            I-391                                                                             Me      CHCH.sub.2 H        O  H    OMe  OMe CH                           I-392                                                                             Me      CHCH.sub.2 H        O  H    Me   OMe CH                           I-393                                                                             Me      CHCH.sub.2 H        O  H    Me   OMe N                            I-394                                                                             Me      CHCHMe     H        O  H    OMe  OMe CH                           I-395                                                                             Me      CHCHMe     H        O  H    Me   OMe CH                           I-396                                                                             Me      CHCHMe     H        O  H    Me   OMe N                            I-397                                                                             Me      CCH        H        O  H    OMe  OMe CH                           I-398                                                                             Me      CCH        H        O  H    Me   OMe CH                           I-399                                                                             Me      CCH        H        O  H    Me   OMe N                            I-400                                                                             Me      CCMe       H        O  H    OMe  OMe CH                           I-401                                                                             Me      CCMe       H        O  H    Me   OMe CH                           I-402                                                                             Me      CCMe       H        O  H    Me   OMe N                            I-403                                                                             Me      CHCHCOOMe  H        O  H    OMe  OMe CH                           I-404                                                                             Me      CHCHCOOMe  H        O  H    Me   OMe CH                           I-405                                                                             Me      CHCHCOOMe  H        O  H    Me   OMe N                            I-406                                                                             Me      CH(Me)COMe H        O  H    OMe  OMe CH                           I-407                                                                             Me      CH(Me)COMe H        O  H    Me   OMe CH                           I-408                                                                             Me      CH(Me)COMe H        O  H    Me   OMe N                            I-409                                                                             Me      CH(Me)COEt H        O  H    OMe  OMe CH                           I-410                                                                             Me      CH(Me)COEt H        O  H    Me   OMe CH                           I-411                                                                             Me      CH(Me)COEt H        O  H    Me   OMe N                            I-412                                                                             Me      CH(Et)COMe H        O  H    OMe  OMe CH                           I-413                                                                             Me      CH(Et)COMe H        O  H    Me   OMe CH                           I-414                                                                             Me      CH(Et)COMe H        O  H    Me   OMe N                            I-415                                                                             Me      CH(Et)COEt H        O  H    OMe  OMe CH                           I-416                                                                             Me      CH(Et)COEt H        O  H    Me   OMe CH                           I-417                                                                             Me      CH(Et)COEt H        O  H    Me   OMe N                            I-418                                                                             Me                                                                                     ##STR8##  H        O  H    OMe  OMe CH                           I-419                                                                             Me                                                                                     ##STR9##  H        O  H    Me   OMe CH                           I-420                                                                             Me                                                                                     ##STR10## H        O  H    Me   OMe N                            I-421                                                                             Me      COPr       H        O  H    OMe  OMe CH                           I-422                                                                             Me      COPr       H        O  H    Me   OMe CH                           I-423                                                                             Me      COPr       H        O  H    Me   OMe N                            I-424                                                                             Me      COPr-i     H        O  H    OMe  OMe CH                           I-425                                                                             Me      COPr-i     H        O  H    Me   OMe CH                           I-426                                                                             Me      COPr-i     H        O  H    Me   OMe N                            I-427                                                                             Me      CHNOMe     H        O  H    OMe  OMe CH                           I-428                                                                             Me      CHNOMe     H        O  H    Me   OMe CH                           I-429                                                                             Me      CHNOMe     H        O  H    Me   OMe N                            I-430                                                                             Me      CHNOEt     H        O  H    OMe  OMe CH                           I-431                                                                             Me      CHNOEt     H        O  H    Me   OMe CH                           I-432                                                                             Me      CHNOEt     H        O  H    Me   OMe N                            I-433                                                                             Me      C(Me)NOMe  H        O  H    OMe  OMe CH                           I-434                                                                             Me      C(Me)NOMe  H        O  H    Me   OMe CH                           I-435                                                                             Me      C(Me)NOMe  H        O  H    Me   OMe N                            I-436                                                                             Me      C(Me)NOEt  H        O  H    OMe  OMe CH                           I-437                                                                             Me      C(Me)NOEt  H        O  H    Me   OMe CH                           I-438                                                                             Me      C(Me)NOEt  H        O  H    Me   OMe N                            I-439                                                                             Me      C(Me)NOPr  H        O  H    OMe  OMe CH                           I-440                                                                             Me      C(Me)NOPr  H        O  H    Me   OMe CH                           I-441                                                                             Me      C(Me)NOPr  H        O  H    Me   OMe N                            I-442                                                                             Me      C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O  H    OMe  OMe CH                           I-443                                                                             Me      C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O  H    Me   OMe CH                           I-444                                                                             Me      C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O  H    Me   OMe N                            I-445                                                                             Me      C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O  H    OMe  OMe CH                           I-446                                                                             Me      C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O  H    Me   OMe CH                           I-447                                                                             Me      C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O  H    Me   OMe N                            I-448                                                                             Me      NHEt       H        O  H    OMe  OMe CH                           I-449                                                                             Me      NHEt       H        O  H    Me   OMe CH                           I-450                                                                             Me      NHEt       H        O  H    Me   OMe N                            I-451                                                                             Me      NHPr       H        O  H    OMe  OMe CH                           I-452                                                                             Me      NHPr       H        O  H    Me   OMe CH                           I-453                                                                             Me      NHPr       H        O  H    Me   OMe N                            I-454                                                                             Me      NHCOOMe    H        O  H    OMe  OMe CH                           I-455                                                                             Me      NHCOOMe    H        O  H    Me   OMe CH                           I-456                                                                             Me      NHCOOMe    H        O  H    Me   OMe N                            I-457                                                                             Me      NHCOOEt    H        O  H    OMe  OMe CH                           I-458                                                                             Me      NHCOOEt    H        O  H    Me   OMe CH                           I-459                                                                             Me      NHCOOEt    H        O  H    Me   OMe N                            I-460                                                                             Me      NHCOOPh    H        O  H    OMe  OMe CH                           I-461                                                                             Me      NHCOOPh    H        O  H    Me   OMe CH                           I-462                                                                             Me      NHCOOPh    H        O  H    Me   OMe N                            I-463                                                                             Me      N(Me)SO.sub.2 Me                                                                         H        O  H    OMe  OMe CH                           I-464                                                                             Me      N(Me)SO.sub.2 Me                                                                         H        O  H    Me   OMe CH                           I-465                                                                             Me      N(Me)SO.sub.2 Me                                                                         H        O  H    Me   OMe N                            I-466                                                                             Me      N(Et)SO.sub.2 Me                                                                         H        O  H    OMe  OMe CH                           I-467                                                                             Me      N(Et)SO.sub.2 Me                                                                         H        O  H    Me   OMe CH                           I-468                                                                             Me      N(Et)SO.sub.2 Me                                                                         H        O  H    Me   OMe N                            I-469                                                                             Me      N(Me)SO.sub.2 Et                                                                         H        O  H    OMe  OMe CH                           I-470                                                                             Me      N(Me)SO.sub.2 Et                                                                         H        O  H    Me   OMe CH                           I-471                                                                             Me      N(Me)SO.sub.2 Et                                                                         H        O  H    OMe  OMe N                            I-472                                                                             Me      N(Et)SO.sub.2 Et                                                                         H        O  H    OMe  OMe CH                           I-473                                                                             Me      N(Et)SO.sub.2 Et                                                                         H        O  H    Me   OMe CH                           I-474                                                                             Me      N(Et)SO.sub.2 Et                                                                         H        O  H    Me   OMe N                            I-475                                                                             Me      NHCOEt     H        O  H    OMe  OMe CH                           I-476                                                                             Me      NHCOEt     H        O  H    Me   OMe CH                           I-477                                                                             Me      NHCOEt     H        O  H    Me   OMe N                            I-478                                                                             Me      NHCOCF.sub.3                                                                             H        O  H    OMe  OMe CH                           I-479                                                                             Me      NHCOCF.sub.3                                                                             H        O  H    Me   OMe CH                           I-480                                                                             Me      NHCOCF.sub.3                                                                             H        O  H    Me   OMe N                            I-481                                                                             Me      NCHMe      H        O  H    OMe  OMe CH                           I-482                                                                             Me      NCHMe      H        O  H    Me   OMe CH                           I-483                                                                             Me      NCHMe      H        O  H    Me   OMe N                            I-484                                                                             Me      NCHPh      H        O  H    OMe  OMe CH                           I-485                                                                             Me      NCHPh      H        O  H    Me   OMe CH                           I-486                                                                             Me      NCHPh      H        O  H    Me   OMe N                            I-487                                                                             Me      N.sub.3    H        O  H    OMe  OMe CH                           I-488                                                                             Me      N.sub.3    H        O  H    Me   OMe CH                           I-489                                                                             Me      N.sub.3    H        O  H    Me   OMe N                            I-490                                                                             Me      I          H        O  H    OMe  OMe CH                           I-491                                                                             Me      I          H        O  H    Me   OMe CH                           I-492                                                                             Me      I          H        O  H    Me   OMe N                            I-493                                                                             Me      OCOEt      H        O  H    OMe  OMe CH                           I-494                                                                             Me      OCOEt      H        O  H    Me   OMe CH                           I-495                                                                             Me      OCOEt      H        O  H    Me   OMe N                            I-496                                                                             Me      OCOPr      H        O  H    OMe  OMe CH                           I-497                                                                             Me      OCOPr      H        O  H    Me   OMe CH                           I-498                                                                             Me      OCOPr      H        O  H    Me   OMe N                            I-499                                                                             Me      OCOPh      H        O  H    OMe  OMe CH                           I-500                                                                             Me      OCOPh      H        O  H    Me   OMe CH                           I-501                                                                             Me      OCOPh      H        O  H    Me   OMe N                            I-502                                                                             Me      OCONMe.sub.2                                                                             H        O  H    OMe  OMe CH                           I-503                                                                             Me      OCONMe.sub.2                                                                             H        O  W    Me   OMe CH                           I-504                                                                             Me      OCONMe.sub.2                                                                             H        O  H    Me   OMe N                            I-505                                                                             Me      Cl         H        O  H    CF.sub.3                                                                           OMe CH                           I-506                                                                             Me      OPr-i      H        O  H    Cl   OMe CH 163-165                   I-507                                                                             Me      SEt        H        O  H    Me   OMe CH 225-227                   I-508                                                                             Me      SEt        H        O  H    Cl   OMe CH 185-187                   I-509                                                                             Me      SEt        H        O  H    Me   Me  CH 220-222                   I-510                                                                             Me      SEt        H        O  H    OMe  OMe N  173-175                   I-511                                                                             Me      SBu        H        O  H    OMe  Me  CH 157-160                   I-512                                                                             Me      SBu        H        O  H    OMe  Me  N  155-157                   I-513                                                                             Me      SPr-i      H        O  H    OMe  Me  CH 185-187                   I-514                                                                             Me      SPr-i      H        O  H    OMe  Me  N  228-229                   I-515                                                                             Me      SOEt       H        O  H    OMe  OMe N  180-182                   I-516                                                                             Me      SO.sub.2 Et                                                                              H        O  H    OMe  Me  CH 270-272                   I-517                                                                             Me      SO.sub.2 Et                                                                              H        O  H    OMe  Me  N  165-168                   I-518                                                                             Me      SO.sub.2 Et                                                                              H        O  H    OMe  Cl  CH 272-275                   I-519                                                                             Me      SO.sub.2 Pr                                                                              H        O  H    OMe  Me  CH 265-267                   I-520                                                                             Me      SO.sub.2 Pr                                                                              H        O  H    OMe  Me  N  132-135                   I-521                                                                             Me      SO.sub.2 Pr                                                                              H        O  H    OMe  Cl  CH 142-145                   I-522                                                                             Me      SO.sub.2 Bu                                                                              H        O  H    OMe  Me  CH 243-246                   I-523                                                                             Me      SO.sub.2 Bu                                                                              H        O  H    OMe  Me  N  241-243                   I-524                                                                             Me      SO.sub.2 Bu                                                                              H        O  H    OMe  Cl  CH 245-247                   I-525                                                                             Me      SO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  CH 135-139                   I-526                                                                             Me      SO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  N  281-282                   I-527                                                                             Me      COOPr      H        O  H    OMe  Me  N  187-189                   I-528                                                                             Me      NO.sub.2   H        O  H    OMe  Cl  CH 204-206                   I-529                                                                             Me      CONMe.sub.2                                                                              H        O  H    OMe  Me  CH 161-164                   I-530                                                                             Me      Br         H        O  H    OMe  Cl  CH 276-279                   I-531                                                                             Me                                                                                     ##STR11## H        O  H    OMe  OMe CH                           I-532                                                                             Me      OCH.sub.2Bu-t                                                                            H        O  H    OMe  OMe CH                           I-533                                                                             Me      OCH.sub.2Bu-t                                                                            H        O  H    Me   OMe CH                           I-534                                                                             Me      OCH.sub.2 CHCMe.sub.2                                                                    H        O  H    OMe  OMe CH                           I-535                                                                             Me      OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O  H    OMe  OMe CH                           I-536                                                                             Me      OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O  H    Me   OMe CH                           I-537                                                                             Me      OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O  H    Me   OMe N                            I-538                                                                             Me      CH.sub.2 CH.sub.2 N.sub.3                                                                H        O  H    OMe  OMe CH                           I-539                                                                             Me                                                                                     ##STR12## H        O  H    OMe  OMe CH                           I-540                                                                             Me      COCF.sub.3 H        O  H    OMe  OMe CH                           I-541                                                                             Me      COOCH.sub.2 CHCHCl                                                                       H        O  H    OMe  OMe CH                           I-542                                                                             Me      SO.sub.2 CF.sub.3                                                                        H        O  H    OMe  OMe CH                           I-543                                                                             Me      OCOCF.sub.3                                                                              H        O  H    OMe  OMe CH                           I-544                                                                             Me      OCH.sub.2 OPh                                                                            H        O  H    OMe  OMe CH                           I-545                                                                             Me      CHNOH      H        O  H    OMe  OMe CH                           I-546                                                                             Me      CHNOCH.sub.2 CHCH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-547                                                                             Me      CHNOCH.sub.2 CCH                                                                         H        O  H    OMe  OMe CH                           I-548                                                                             Me      C(Me)NOBn  H        O  H    OMe  OMe CH                           I-549                                                                             Me      C(Me)NOPh  H        O  H    OMe  OMe CH                           I-550                                                                             Me      C(Bn)NOMe  H        O  H    OMe  OMe CH                           I-551                                                                             Me      C(Ph)NOMe  H        O  H    OMe  OMe CH                           I-552                                                                             Me      C(CF.sub.3)NOMe                                                                          H        O  H    OMe  OMe CH                           I-553                                                                             Me      COOCH.sub.2 CH.sub.2 Cl                                                                  H        O  H    OMe  OMe CH                           I-554                                                                             Me      COOCH.sub.2 CF.sub.3                                                                     H        O  H    OMe  OMe CH                           I-555                                                                             Me      Cl         5-Cl     O  H    OMe  Me  N  182-184                   I-556                                                                             Me      Cl         5-OMe    O  H    OMe  OMe CH                           I-557                                                                             Me      Cl         5-F      O  H    OMe  OMe CH                           I-558                                                                             Me      F          5-Cl     O  H    OMe  OMe CH                           I-559                                                                             Me      F          5-F      O  H    OMe  OMe CH                           I-560                                                                             Me      COOMe      5-Cl     O  H    OMe  OMe CH                           I-561                                                                             Me      COOEt      5-Cl     O  H    OMe  OMe CH                           I-562                                                                             Me      COOPr      5-Cl     O  H    OMe  OMe CH                           I-563                                                                             Me      COOPr-i    5-Cl     O  H    OMe  OMe CH                           I-564                                                                             Me      OMe        5-COOMe  O  H    OMe  OMe CH                           I-565                                                                             Me      COOMe      5-OMe    O  H    OMe  OMe CH                           I-566                                                                             Me      H          5-CN     O  H    OMe  OMe CH                           I-567                                                                             Me      H          5-CF.sub.3                                                                             O  H    OMe  OMe CH                           I-568                                                                             Me      H          5-COOMe  O  H    OMe  OMe CH 235-236                   I-569                                                                             Me      H          5-COOEt  O  H    OMe  OMe CH                           I-570                                                                             Me      H          5-COOPr  O  H    OMe  OMe CH                           I-571                                                                             Me      H          5-COOPr-i                                                                              O  H    OMe  OMe CH                           I-572                                                                             Me      H          5-COOCH.sub.2 CH.sub.2 Cl                                                              O  H    OMe  OMe CH                           I-573                                                                             Me      H          5-COOCH.sub.2 CH.sub.2 F                                                               O  H    OMe  OMe CH                           I-574                                                                             Me      H          5-COOCH.sub.2 CF.sub.3                                                                 O  H    OMe  OMe CH                           I-575                                                                             Me      H          5-COOCH.sub.2 OMe                                                                      O  H    OMe  OMe CH                           I-576                                                                             Me      H          5-CONMe.sub.2                                                                          O  H    OMe  OMe CH                           I-577                                                                             Me      H          5-OCH.sub.2 CH.sub.2 F                                                                 O  H    OMe  OMe CH                           I-578                                                                             Me      H          5-OCHF.sub.2                                                                           O  H    OMe  OMe CH                           I-579                                                                             Me      H          5-OCH.sub.2 CF.sub.3                                                                   O  H    OMe  OMe CH                           I-580                                                                             Me      H          5-OCH.sub.2 CH.sub.2 CH.sub.2 F                                                        O  H    OMe  OMe CH                           I-581                                                                             Me      H          5-OCH.sub.2 CHCH.sub.2                                                                 O  H    OMe  OMe CH                           I-582                                                                             Me      H          5-OCH.sub.2 CCH                                                                        O  H    OMe  OMe CH                           I-583                                                                             Me      H          5-NO.sub.2                                                                             O  H    OMe  OMe CH                           I-584                                                                             Me      H          5-SMe    O  H    OMe  OMe CH                           I-585                                                                             Me      H          5-SEt    O  H    OMe  OMe CH                           I-586                                                                             Me      H          5-SPr    O  H    OMe  OMe CH                           I-587                                                                             Me      H          5-SPr-i  O  H    OMe  OMe CH                           I-588                                                                             Me      H          5-SO.sub.2 Et                                                                          O  H    OMe  OMe CH                           I-589                                                                             Me      H          5-SO.sub.2 Pr                                                                          O  H    OMe  OMe CH                           I-590                                                                             Me      H          5-SO.sub.2 Pr-i                                                                        O  H    OMe  OMe CH                           I-591                                                                             Me      H          5-SOEt   O  H    OMe  OMe CH                           I-592                                                                             Me      H          5-Me     O  H    OMe  OMe CH                           I-593                                                                             Me      H          5-Et     O  H    OMe  OMe CH                           I-594                                                                             Me      H          5-Pr     O  H    OMe  OMe CH                           I-595                                                                             Me      H          5-SO.sub.2 NMe.sub.2                                                                   O  H    OMe  OMe CH                           I-596                                                                             Me      H          5-OCF.sub.3                                                                            O  H    OMe  OMe CH                           I-597                                                                             Me      H          5-CH.sub.2 CF.sub.3                                                                    O  H    OMe  OMe CH                           I-598                                                                             Me      H          5-CH.sub.2 CHCH.sub.2                                                                  O  H    OMe  OMe CH                           I-599                                                                             Me      H          5-COOMe  O  H    OMe  Me  CH 134-135                   I-600                                                                             Me      H          5-COOMe  O  H    OMe  Me  N  143-144                   I-601                                                                             Me      H          5-COOMe  O  H    OMe  OMe N  148-150                   I-602                                                                             Me                                                                                     ##STR13## H        O  H    OMe  OMe CH                           I-603                                                                             Me                                                                                     ##STR14## H        O  H    Me   OMe CH                           I-604                                                                             Me                                                                                     ##STR15## H        O  H    Me   OMe N                            I-605                                                                             Me                                                                                     ##STR16## H        O  H    OMe  OMe CH                           I-606                                                                             Me                                                                                     ##STR17## H        O  H    Me   OMe CH                           I-607                                                                             Me                                                                                     ##STR18## H        O  H    Me   OMe N                            I-608                                                                             Me                                                                                     ##STR19## H        O  H    OMe  OMe CH                           I-609                                                                             Me                                                                                     ##STR20## H        O  H    Me   OMe CH                           I-610                                                                             Me                                                                                     ##STR21## H        O  H    Me   OMe N                            I-611                                                                             Me      OC.sub.2 H.sub.4O*  O  H    OMe  OMe CH                           I-612                                                                             Me      OC.sub.2 H.sub.4O*  O  H    Me   OMe CH                           I-613                                                                             Me      OC.sub.2 H.sub.4O*  O  H    Me   OMe N                            I-614                                                                             Me      SC.sub.2 H.sub.4S*  O  H    OMe  OMe CH                           I-615                                                                             Me      SC.sub.2 H.sub.4S*  O  H    Me   OMe CH                           I-616                                                                             Me      SC.sub.2 H.sub.4S*  O  H    Me   OMe N                            I-617                                                                             Me      OCH.sub.2O*         O  H    OMe  OMe CH                           I-618                                                                              ##STR22##                                                                            Cl         H        O  H    OMe  OMe CH                           I-619                                                                              ##STR23##                                                                            Cl         H        O  H    OMe  OMe CH                           I-620                                                                              ##STR24##                                                                            Cl         H        O  H    OMe  OMe CH                           I-621                                                                             COMe    Cl         H        O  H    OMe  OMe CH                           I-622                                                                             COEt    Cl         H        O  H    OMe  OMe CH                           I-623                                                                             COPr    Cl         H        O  H    OMe  OMe CH                           I-624                                                                             COPr-i  Cl         H        O  H    OMe  OMe CH                           I-625                                                                             COPh    Cl         H        O  H    OMe  OMe CH                           I-626                                                                             SO.sub.2 Me                                                                           Cl         H        O  H    OMe  OMe CH                           I-627                                                                             SO.sub.2 Et                                                                           Cl         H        O  H    OMe  OMe CH                           I-628                                                                             SO.sub.2 Ph                                                                           Cl         H        O  H    OMe  OMe CH                           I-629                                                                             COOMe   Cl         H        O  H    OMe  OMe CH                           I-630                                                                             COOEt   Cl         H        O  H    OMe  OMe CH                           I-631                                                                             COOPh   Cl         H        O  H    OMe  OMe CH                           I-632                                                                             CONMe.sub.2                                                                           Cl         H        O  H    OMe  OMe CH                           I-633                                                                             SO.sub.2 NMe.sub.2                                                                    Cl         H        O  H    OMe  OMe CH                           I-634                                                                             Ph      Cl         H        O  H    Me   OMe N                            I-635                                                                             CH.sub.2 OMe                                                                          Cl         H        O  H    OMe  OMe CH                           I-636                                                                             CH.sub.2 OBn                                                                          Cl         H        O  H    OMe  OMe CH                           I-637                                                                             CH.sub.2 CH.sub.2 F                                                                   Cl         H        O  H    OMe  OMe CH                           I-638                                                                             CH.sub.2 CH.sub.2 Cl                                                                  Cl         H        O  H    OMe  OMe CH                           I-639                                                                             CF.sub.3                                                                              Cl         H        O  H    OMe  OMe CH                           I-640                                                                             CH.sub.2 F                                                                            Cl         H        O  H    OMe  OMe CH                           I-641                                                                             CH.sub.2 CHCH.sub.2                                                                   OMe        H        O  H    OMe  OMe CH 221-223                   I-642                                                                             COCF.sub.3                                                                            Cl         H        O  H    OMe  OMe CH                           I-643                                                                              ##STR25##                                                                            Cl         H        O  H    OMe  OMe CH                           I-644                                                                             H       Bn         H        O  H    OMe  OMe CH                           I-645                                                                             H       Br         H        O  H    OMe  Me  CH 183-184                   I-646                                                                             H       Br         H        O  H    OMe  Me  N  154-155                   I-647                                                                             H       Br         H        O  H    OMe  OMe CH                           I-648                                                                             H       Bu         H        O  H    Me   OMe CH                           I-649                                                                             H       Bu         H        O  H    Me   OMe N                            I-650                                                                             H       Bu         H        O  H    OMe  OMe CH                           I-651                                                                             H       Bu-t       H        O  H    Me   OMe CH                           I-652                                                                             H       Bu-t       H        O  H    Me   OMe N                            I-653                                                                             H       Bu-t       H        O  H    OMe  OMe CH                           I-654                                                                             H       C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O  H    Me   OMe CH                           I-655                                                                             H       C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O  H    Me   OMe N                            I-656                                                                             H       C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O  H    OMe  OMe CH                           I-657                                                                             H       C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O  H    Me   OMe CH                           I-658                                                                             H       C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O  H    Me   OMe N                            I-659                                                                             H       C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O  H    OMe  OMe CH                           I-660                                                                             H       C(Me)NOEt  H        O  H    Me   OMe CH                           I-661                                                                             H       C(Me)NOEt  H        O  H    Me   OMe N                            I-662                                                                             H       C(Me)NOEt  H        O  H    OMe  OMe CH                           I-663                                                                             H       C(Me)NOMe  H        O  H    Me   OMe CH                           I-664                                                                             H       C(Me)NOMe  H        O  H    Me   OMe N                            I-665                                                                             H       C(Me)NOMe  H        O  H    OMe  OMe CH                           I-666                                                                             H       C(Me)NOPr  H        O  H    Me   OMe CH                           I-667                                                                             H       C(Me)NOPr  H        O  H    Me   OMe N                            I-668                                                                             H       C(Me)NOPr  H        O  H    OMe  OMe CH                           I-669                                                                             H       CCH        H        O  H    Me   OMe CH                           I-670                                                                             H       CCH        H        O  H    Me   OMe N                            I-671                                                                             H       CCH        H        O  H    OMe  OMe CH                           I-672                                                                             H       CCMe       H        O  H    Me   OMe CH                           I-673                                                                             H       CCMe       H        O  H    Me   OMe N                            I-674                                                                             H       CCMe       H        O  H    OMe  OMe CH                           I-675                                                                             H       CF.sub.3   H        O  H    OMe  OMe CH                           I-676                                                                             H       CH(Et)COEt H        O  H    Me   OMe CH                           I-677                                                                             H       CH(Et)COEt H        O  H    Me   OMe N                            I-678                                                                             H       CH(Et)COEt H        O  H    OMe  OMe CH                           I-679                                                                             H       CH(Et)COMe H        O  H    Me   OMe CH                           I-680                                                                             H       CH(Et)COMe H        O  H    Me   OMe N                            I-681                                                                             H       CH(Et)COMe H        O  H    OMe  OMe CH                           I-682                                                                             H       CH(Me)COEt H        O  H    Me   OMe CH                           I-683                                                                             H       CH(Me)COEt H        O  H    Me   OMe N                            I-684                                                                             H       CH(Me)COEt H        O  H    OMe  OMe CH                           I-685                                                                             H       CH(Me)COMe H        O  H    Me   OMe CH                           I-686                                                                             H       CH(Me)COMe H        O  H    Me   OMe N                            I-687                                                                             H       CH(Me)COMe H        O  H    OMe  OMe CH                           I-688                                                                             H       CHCHCOOMe  H        O  H    Me   OMe CH                           I-689                                                                             H       CHCHCOOMe  H        O  H    Me   OMe N                            I-690                                                                             H       CHCHCOOMe  H        O  H    OMe  OMe CH                           I-691                                                                             H       CHCH.sub.2 H        O  H    Me   OMe CH                           I-692                                                                             H       CHCH.sub.2 H        O  H    Me   OMe N                            I-693                                                                             H       CHCH.sub.2 H        O  H    OMe  OMe CH                           I-694                                                                             H       CHCHMe     H        O  H    Me   OMe CH                           I-695                                                                             H       CHCHMe     H        O  H    Me   OMe N                            I-696                                                                             H       CHCHMe     H        O  H    OMe  OMe CH                           I-697                                                                             H       CHNOEt     H        O  H    Me   OMe CH                           I-698                                                                             H       CHNOEt     H        O  H    Me   OMe N                            I-699                                                                             H       CHNOEt     H        O  H    OMe  OMe CH                           I-700                                                                             H       CHNOMe     H        O  H    Me   OMe CH                           I-701                                                                             H       CHNOMe     H        O  H    Me   OMe N                            I-702                                                                             H       CHNOMe     H        O  H    OMe  OMe CH                           I-703                                                                             H       CH.sub.2 CCH                                                                             H        O  H    Me   OMe CH                           I-704                                                                             H       CH.sub.2 CCH                                                                             H        O  H    Me   OMe N                            I-705                                                                             H       CH.sub.2 CCH                                                                             H        O  H    OMe  OMe CH                           I-706                                                                             H       CH.sub.2 CF.sub.3                                                                        H        O  H    Me   OMe CH                           I-707                                                                             H       CH.sub.2 CF.sub.3                                                                        H        O  H    Me   OMe N                            I-708                                                                             H       CH.sub.2 CF.sub.3                                                                        H        O  H    OMe  OMe CH                           I-709                                                                             H       CH.sub.2 CHCH.sub.2                                                                      H        O  H    Me   OMe CH                           I-710                                                                             H       CH.sub.2 CHCH.sub.2                                                                      H        O  H    Me   OMe N                            I-711                                                                             H       CH.sub.2 CHCH.sub.2                                                                      H        O  H    OMe  OMe CH                           I-712                                                                             H       CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O  H    Me   OMe CH                           I-713                                                                             H       CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O  H    Me   OMe N                            I-714                                                                             W       CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O  H    OMe  OMe CH                           I-715                                                                             H       CH.sub.2 CN                                                                              H        O  H    Me   OMe CH                           I-716                                                                             H       CH.sub.2 CN                                                                              H        O  H    Me   OMe N                            I-717                                                                             H       CH.sub.2 CN                                                                              H        O  H    OMe  OMe CH                           I-718                                                                             H       CH.sub.2 CONMe.sub.2                                                                     H        O  H    Me   OMe CH                           I-719                                                                             H       CH.sub.2 CONMe.sub.2                                                                     H        O  H    Me   OMe N                            I-720                                                                             H       CH.sub.2 CONMe.sub.2                                                                     H        O  H    OMe  OMe CH                           I-721                                                                             H       CH.sub.2 COOEt                                                                           H        O  H    Me   OMe CH                           I-722                                                                             H       CH.sub.2 COOEt                                                                           H        O  H    Me   OMe N                            I-723                                                                             H       CH.sub.2 COOEt                                                                           H        O  H    OMe  OMe CH                           I-724                                                                             H       CH.sub.2 COOMe                                                                           H        O  H    Me   OMe CH                           I-725                                                                             H       CH.sub.2 COOMe                                                                           H        O  H    Me   OMe N                            I-726                                                                             H       CH.sub.2 COOMe                                                                           H        O  H    OMe  OMe CH                           I-727                                                                             H       CH.sub.2 Cl                                                                              H        O  H    Me   OMe CH                           I-728                                                                             H       CH.sub.2 Cl                                                                              H        O  H    Me   OMe N                            I-729                                                                             H       CH.sub.2 Cl                                                                              H        O  H    OMe  OMe CH                           I-730                                                                             H       CH.sub.2 F H        O  H    Me   OMe CH                           I-731                                                                             H       CH.sub.2 F H        O  H    Me   OMe N                            I-732                                                                             H       CH.sub.2 F H        O  H    OMe  OMe CH                           I-733                                                                             H       CH.sub.2 NMe.sub.2                                                                       H        O  H    Me   OMe CH                           I-734                                                                             H       CH.sub.2 NMe.sub.2                                                                       H        O  H    Me   OMe N                            I-735                                                                             H       CH.sub.2 NMe.sub.2                                                                       H        O  H    OMe  OMe CH                           I-736                                                                             H       CH.sub.2 OMe                                                                             H        O  H    Me   OMe CH                           I-737                                                                             H       CH.sub.2 OMe                                                                             H        O  H    Me   OMe N                            I-738                                                                             H       CH.sub.2 OMe                                                                             H        O  H    OMe  OMe CH                           I-739                                                                             H       CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O  H    Me   OMe CH                           I-740                                                                             H       CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O  H    Me   OMe N                            I-741                                                                             H       CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O  H    OMe  OMe CH                           I-742                                                                             H       CN         H        O  H    OMe  Me  CH                           I-743                                                                             H       CN         H        O  H    OMe  Me  N                            I-744                                                                             H       CN         H        O  H    OMe  OMe CH                           I-745                                                                             H                                                                                      ##STR26## H        O  H    Me   OMe CH                           I-746                                                                             H                                                                                      ##STR27## H        O  H    Me   OMe N                            I-747                                                                             H                                                                                      ##STR28## H        O  H    OMe  OMe CH                           I-748                                                                             H       CO.sub.2 Bn                                                                              H        O  H    OMe  OMe CH                           I-749                                                                             H       CO.sub.2 Bu                                                                              H        O  H    OMe  Me  CH                           I-750                                                                             H       CO.sub.2 Bu                                                                              H        O  H    OMe  Me  N                            I-751                                                                             H       CO.sub.2 Bu                                                                              H        O  H    OMe  OMe CH                           I-752                                                                             H       CO.sub.2 CH.sub.2 CCH                                                                    H        O  H    OMe  OMe CH                           I-753                                                                             H       CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    OMe  OMe CH                           I-754                                                                             H       CO.sub.2 CH.sub.2 CH.sub.2 F                                                             H        O  H    OMe  OMe CH                           I-755                                                                             H       CO.sub.2 Et                                                                              H        O  H    OCHF.sub.2                                                                         OCHF.sub.2                                                                        CH                           I-756                                                                             H       CO.sub.2 Et                                                                              H        O  H    OMe  Me  N                            I-757                                                                             H       CO.sub.2 Et                                                                              H        S  H    OMe  OMe CH                           I-758                                                                             H       CO.sub.2 H H        O  H    OMe  OMe CH                           I-759                                                                             H       CO.sub.2 Me                                                                              5-F      O  H    OMe  OMe CH                           I-760                                                                             H       CO.sub.2 Me                                                                              H        O  H    OCHF.sub.2                                                                         OCHF.sub.2                                                                        CH                           I-761                                                                             H       CO.sub.2 Me                                                                              H        O  H    OMe  Me  CH 202-205                   I-762                                                                             H       CO.sub.2 Me                                                                              H        O  H    OMe  Me  N  169-170                   I-763                                                                             H       CO.sub.2 Me                                                                              H        O  H    OMe  OCHF.sub.2                                                                        CH                           I-764                                                                             H       CO.sub.2 Me                                                                              H        O  Me   OMe  OMe CH                           I-765                                                                             H       CO.sub.2 Me                                                                              H        S  H    OMe  OMe CH                           I-766                                                                             H       CO.sub.2 Pen                                                                             H        O  H    OMe  OMe CH                           I-767                                                                             H       CO.sub.2 Ph                                                                              H        O  H    OMe  OMe CH                           I-768                                                                             H       CO.sub.2 Pr                                                                              H        O  H    OMe  Me  CH                           I-769                                                                             H       CO.sub.2 Pr                                                                              H        O  H    OMe  OMe CH                           I-770                                                                             H       CO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  CH                           I-771                                                                             H       CO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  N                            I-772                                                                             H       CO.sub.2 Pr-i                                                                            H        O  H    OMe  OMe CH                           I-773                                                                             H       COBn       H        O  H    OMe  OMe CH                           I-774                                                                             H       COCH.sub.2 CCH                                                                           H        O  H    OMe  OMe CH                           I-775                                                                             H       COCH.sub.2 CHCH.sub.2                                                                    H        O  H    OMe  OMe CH                           I-776                                                                             H       COEt       H        O  H    OMe  OMe CH                           I-777                                                                             H       COH        H        O  H    OMe  OMe CH                           I-778                                                                             H       COMe       H        O  H    OMe  OMe CH                           I-779                                                                             H       CON(Et).sub.2                                                                            H        O  H    OMe  OMe CH                           I-780                                                                             H       CON(Me).sub.2                                                                            H        O  H    OMe  OMe CH                           I-781                                                                             H       CONH.sub.2 H        O  H    OMe  OMe CH                           I-782                                                                             H       CONHBn     H        O  H    OMe  OMe CH                           I-783                                                                             H       CONHCH.sub.2 CCH                                                                         H        O  H    OMe  OMe CH                           I-784                                                                             H       CONHCH.sub.2 CHCH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-785                                                                             H       CONHEt     H        O  H    OMe  OMe CH                           I-786                                                                             H       CONHMe     H        O  H    OMe  OMe CH                           I-787                                                                             H       CONHOMe    H        O  H    OMe  OMe CH                           I-788                                                                             H       CONHPh     H        O  H    OMe  OMe CH                           I-789                                                                             H       CONHPr     H        O  H    OMe  OMe CH                           I-790                                                                             H       COOMe      H        O  H    OMe  Me  CH                           I-791                                                                             H       COOMe      H        O  H    Me   OMe N                            I-792                                                                             H       COPh       H        O  H    OMe  OMe CH                           I-793                                                                             H       COPr       H        O  H    Me   OMe CH                           I-794                                                                             H       COPr       H        O  H    Me   OMe N                            I-795                                                                             H       COPr       H        O  H    OMe  OMe CH                           I-796                                                                             H       COPr-i     H        O  H    Me   OMe CH                           I-797                                                                             H       COPr-i     H        O  H    Me   OMe N                            I-798                                                                             H       COPr-i     H        O  H    OMe  OMe CH                           I-799                                                                             H       Cl         5-Cl     O  H    OMe  OMe CH                           I-800                                                                             H       Cl         H        S  H    Cl   OMe CH                           I-801                                                                             H       Cl         H        O  H    Me   Me  CH                           I-802                                                                             H       Cl         H        O  H    OMe  Me  CH                           I-803                                                                             H       Cl         H        O  H    OMe  Me  N                            I-804                                                                             H       Cl         H        S  H    Me   Me  CH                           I-805                                                                             H       Cl         H        S  H    OMe  Me  CH                           I-806                                                                             H       Cl         H        S  H    OMe  Me  N                            I-807                                                                             H       Cl         H        O  Me   OMe  OMe CH                           I-808                                                                             H       Cl         H        S  H    OMe  OMe CH                           I-809                                                                             H       Et         H        O  H    Me   OMe CH                           I-810                                                                             H       Et         H        O  H    Me   OMe N                            I-811                                                                             H       Et         H        O  H    OMe  OMe CH                           I-812                                                                             H       F          H        O  H    Me   Me  CH                           I-813                                                                             H       F          H        O  H    OMe  Me  CH                           I-814                                                                             H       F          H        O  H    OMe  Me  N                            I-815                                                                             H       F          H        O  H    OMe  OMe CH                           I-816                                                                             H       H          5-Cl     O  H    Me   Me  CH                           I-817                                                                             H       H          5-Cl     O  H    OMe  Me  N                            I-818                                                                             H       H          5-Cl     O  H    OMe  OMe CH                           I-819                                                                             H       H          5-F      O  H    Me   Me  CH                           I-820                                                                             H       H          5-F      O  H    OMe  Me  CH                           I-821                                                                             H       H          5-F      O  H    OMe  Me  N                            I-822                                                                             H       H          5-F      O  H    OMe  OMe CH                           I-823                                                                             H       H          5-OEt    O  H    OMe  Me  CH                           I-824                                                                             H       H          5-OEt    O  H    OMe  Me  N                            I-825                                                                             H       H          5-OEt    O  H    OMe  OMe CH                           I-826                                                                             H       H          5-OEt    O  H    OMe  OMe N                            I-827                                                                             H       H          5-OMe    O  H    Cl   OMe CH                           I-828                                                                             H       H          5-OMe    O  H    OMe  Me  CH                           I-829                                                                             H       H          5-OMe    O  H    OMe  Me  N                            I-830                                                                             H       H          5-OMe    O  H    OMe  OMe CH                           I-831                                                                             H       H          5-OPr    O  H    OMe  Me  CH                           I-832                                                                             H       H          5-OPr    O  H    OMe  Me  N                            I-833                                                                             H       H          5-OPr    O  H    OMe  OMe CH                           I-834                                                                             H       H          5-OPr    O  H    OMe  OMe N                            I-835                                                                             H       H          6-Cl     O  H    Me   Me  CH                           I-836                                                                             H       H          6-Cl     O  H    OMe  Me  N                            I-837                                                                             H       H          6-Cl     O  H    OMe  OMe CH                           I-838                                                                             H       H          7-Cl     O  H    OMe  Me  N                            I-839                                                                             H       H          7-Cl     O  H    OMe  OMe CH                           I-840                                                                             H       H          H        O  H    Me   Me  CH                           I-841                                                                             H       H          H        O  H    OMe  Me  N                            I-842                                                                             H       H          H        O  H    OMe  OMe CH                           I-843                                                                             H       I          H        O  H    Me   OMe CH                           I-844                                                                             H       I          H        O  H    Me   OMe N                            I-845                                                                             H       I          H        O  H    OMe  OMe CH                           I-846                                                                             H       Me         H        O  H    OMe  OMe CH                           I-847                                                                             H       N(Et)SO.sub.2 Et                                                                         H        O  H    Me   OMe CH                           I-848                                                                             H       N(Et)SO.sub.2 Et                                                                         H        O  H    Me   OMe N                            I-849                                                                             H       N(Et)SO.sub.2 Et                                                                         H        O  H    OMe  OMe CH                           I-850                                                                             H       N(Et)SO.sub.2 Me                                                                         H        O  H    Me   OMe CH                           I-851                                                                             H       N(Et)SO.sub.2 Me                                                                         H        O  H    Me   OMe N                            I-852                                                                             H       N(Et)SO.sub.2 Me                                                                         H        O  H    OMe  OMe CH                           I-853                                                                             H       N(Me).sub.2                                                                              H        O  H    OMe  OMe CH                           I-854                                                                             H       N(Me)SO.sub.2 Et                                                                         H        O  H    Me   OMe CH                           I-855                                                                             H       N(Me)SO.sub.2 Et                                                                         H        O  H    Me   OMe N                            I-856                                                                             H       N(Me)SO.sub.2 Et                                                                         H        O  H    OMe  OMe CH                           I-857                                                                             H       N(Me)SO.sub.2 Me                                                                         H        O  H    Me   OMe CH                           I-858                                                                             H       N(Me)SO.sub.2 Me                                                                         H        O  H    Me   OMe N                            I-859                                                                             H       N(Me)SO.sub.2 Me                                                                         H        O  H    OMe  OMe CH                           I-860                                                                             H       NCHPh      H        O  H    Me   OMe CH                           I-861                                                                             H       NCHPh      H        O  H    Me   OMe N                            I-862                                                                             H       NCHPh      H        O  H    OMe  OMe CH                           I-863                                                                             H       NCHMe      H        O  H    Me   OMe CH                           I-864                                                                             H       NCHMe      H        O  H    Me   OMe N                            I-865                                                                             N       NCHMe      H        O  H    OMe  OMe CH                           I-866                                                                             H       N.sub.3    H        O  H    Me   OMe CH                           I-867                                                                             H       N.sub.3    H        O  H    Me   OMe N                            I-868                                                                             H       N.sub.3    H        O  H    OMe  OMe CH                           I-869                                                                             H       NEt.sub.2  H        O  H    OMe  OMe CH                           I-870                                                                             H       NH.sub.2   H        O  H    OMe  OMe CH                           I-871                                                                             H       NHBn       H        O  H    Cl   OMe CH                           I-872                                                                             H       NHBn       H        O  H    OMe  OMe CH                           I-873                                                                             H       NHCOCF.sub.3                                                                             H        O  H    Me   OMe CH                           I-874                                                                             H       NHCOCF.sub.3                                                                             H        O  H    Me   OMe N                            I-875                                                                             H       NHCOCF.sub.3                                                                             H        O  H    OMe  OMe CH                           I-876                                                                             H       NHCOCH.sub.2 Cl                                                                          H        O  H    OMe  OMe CH                           I-877                                                                             H       NHCOEt     H        O  H    Me   OMe CH                           I-878                                                                             H       NHCOEt     H        O  H    Me   OMe N                            I-879                                                                             H       NHCOEt     H        O  H    OMe  OMe CH                           I-880                                                                             H       NHCOMe     H        O  H    OMe  OMe CH                           I-881                                                                             H       NHCOOEt    H        O  H    Me   OMe CH                           I-882                                                                             H       NHCOOEt    H        O  H    Me   OMe N                            I-883                                                                             H       NHCOOEt    H        O  H    OMe  OMe CH                           I-884                                                                             H       NHCOOMe    H        O  H    Me   OMe CH                           I-885                                                                             H       NHCOOMe    H        O  H    Me   OMe N                            I-886                                                                             H       NHCOOMe    H        O  H    OMe  OMe CH                           I-887                                                                             H       NHCOOPh    H        O  H    Me   OMe CH                           I-888                                                                             H       NHCOOPh    H        O  H    Me   OMe N                            I-889                                                                             H       NHCOOPh    H        O  H    OMe  OMe CH                           I-890                                                                             H       NHCOPh     H        O  H    OMe  OMe CH                           I-891                                                                             H       NHEt       H        O  H    Me   OMe CH                           I-892                                                                             H       NHEt       H        O  H    Me   OMe N                            I-893                                                                             H       NHEt       H        O  H    OMe  OMe CH                           I-894                                                                             N       NHMe       H        O  H    OMe  Me  CH                           I-895                                                                             H       NHMe       H        O  H    OMe  Me  N                            I-896                                                                             H       NHMe       H        O  H    OMe  OMe CH                           I-897                                                                             H       NHPr       H        O  H    Me   OMe CH                           I-898                                                                             H       NHPr       H        O  H    Me   OMe N                            I-899                                                                             H       NHPr       H        O  H    OMe  OMe CH                           I-900                                                                             H       NHSO.sub.2 CH.sub.3                                                                      H        O  H    OMe  OMe CH                           I-901                                                                             H       NHSO.sub.2 Ph                                                                            H        O  H    OMe  OMe CH                           I-902                                                                             H       NMe.sub.2  H        O  H    Cl   OMe CH                           I-903                                                                             H       NMe.sub.2  H        O  H    Me   Me  CH                           I-904                                                                             H       NMe.sub.2  H        O  H    OMe  Me  N                            I-905                                                                             H       NO.sub.2   H        O  H    OMe  Me  CH 208-210                   I-906                                                                             H       NO.sub.2   H        O  H    OMe  OMe CH 184-186                   I-907                                                                             H       OBn        H        O  H    OMe  OMe CH                           I-908                                                                             H       OBn(2-Me)  H        O  H    OMe  OMe CH                           I-909                                                                             H       OBn(3-OMe) H        O  H    OMe  OMe CH                           I-910                                                                             H       OBn(4-Cl)  H        O  H    OMe  OMe CH                           I-911                                                                             H       OBu        H        O  H    Cl   OMe CH                           I-912                                                                             H       OBu        H        O  H    Me   Me  CH                           I-913                                                                             H       OBu        H        O  H    OMe  Me  CH                           I-914                                                                             H       OBu        H        O  H    OMe  Me  N                            I-915                                                                             H       OBu        H        O  H    OMe  OMe CH                           I-916                                                                             H       OCF.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe CH                           I-917                                                                             H       OCF.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe N                            I-918                                                                             H       OCF.sub.2 CH.sub.2 Cl                                                                    H        O  H    OMe  OMe CH                           I-919                                                                             H       OCF.sub.2 CHFCl                                                                          H        O  H    Me   OMe CH                           I-920                                                                             H       OCF.sub.2 CHFCl                                                                          H        O  H    Me   OMe N                            I-921                                                                             H       OCF.sub.2 CHFCl                                                                          H        O  H    OMe  OMe CH                           I-922                                                                             H       OCF.sub.3  H        O  H    Me   OMe CH                           I-923                                                                             H       OCF.sub.3  H        O  H    Me   OMe N                            I-924                                                                             H       OCF.sub.3  H        O  H    OMe  OMe CH                           I-925                                                                             H       OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O  H    Me   OMe CH                           I-926                                                                             H       OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O  H    Me   OMe N                            I-927                                                                             H       OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O  H    OMe  OMe CH                           I-928                                                                             H       OCH(CF.sub.3)Me                                                                          H        O  H    OMe  Me  CH                           I-929                                                                             H       OCH(CF.sub.3)Me                                                                          H        O  H    OMe  OMe CH                           I-930                                                                             H       OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O  H    Me   OMe CH                           I-931                                                                             H       OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O  H    Me   OMe N                            I-932                                                                             H       OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-933                                                                             H       OCH.sub.2 C(Me)CH.sub.2                                                                  H        O  H    Me   OMe CH                           I-934                                                                             H       OCH.sub.2 C(Me)CH.sub.2                                                                  H        O  H    Me   OMe N                            I-935                                                                             H       OCH.sub.2 C(Me)CH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-936                                                                             H       OCH.sub.2 CCH                                                                            H        O  H    OMe  OMe CH                           I-937                                                                             H       OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O  H    Me   OMe CH                           I-938                                                                             H       OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O  H    Me   OMe N                            I-939                                                                             H       OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O  H    OMe  OMe CH                           I-940                                                                             H       OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O  H    Me   OMe CH                           I-941                                                                             H       OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O  H    Me   OMe N                            I-942                                                                             H       OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O  H    OMe  OMe CH                           I-943                                                                             H       OCH.sub.2 CF.sub.3                                                                       H        O  H    Cl   OMe CH                           I-944                                                                             H       OCH.sub.2 CF.sub.3                                                                       H        O  H    OMe  Me  CH                           I-945                                                                             H       OCH.sub.2 CF.sub.3                                                                       H        O  H    OMe  Me  N                            I-946                                                                             H       OCH.sub.2 CF.sub.3                                                                       H        O  H    OMe  OMe CH                           I-947                                                                             H       OCH.sub.2 CHCCl.sub.2                                                                    H        O  H    Me   OMe CH                           I-948                                                                             H       OCH.sub.2 CHCCl.sub.2                                                                    H        O  H    Me   OMe N                            I-949                                                                             H       OCH.sub.2 CHCCl.sub.2                                                                    H        O  H    OMe  OMe CH                           I-950                                                                             H       OCH.sub.2 CHCHCl                                                                         H        O  H    Me   OMe CH                           I-951                                                                             H       OCH.sub.2 CHCHCl                                                                         H        O  H    Me   OMe N                            I-952                                                                             H       OCH.sub.2 CHCHCl                                                                         H        O  H    OMe  OMe CH                           I-953                                                                             H       OCH.sub.2 CHCH.sub.2                                                                     H        O  H    OMe  OMe CH                           I-954                                                                             H       OCH.sub.2 CHCHMe                                                                         H        O  H    Me   OMe CH                           I-955                                                                             H       OCH.sub.2 CHCHMe                                                                         H        O  H    Me   OMe N                            I-956                                                                             H       OCH.sub.2 CHCHMe                                                                         H        O  H    OMe  OMe CH                           I-957                                                                             H       OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O  H    Me   OMe CH                           I-958                                                                             H       OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O  H    Me   OMe N                            I-959                                                                             H       OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O  H    OMe  OMe CH                           I-960                                                                             H       OCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    OMe  OMe CH                           I-961                                                                             H       OCH.sub.2 CH.sub.2 F                                                                     H        O  H    OMe  OMe CH                           I-962                                                                             H       OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O  H    Me   OMe CH                           I-963                                                                             H       OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O  H    Me   OMe N                            I-964                                                                             H       OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O  H    OMe  OMe CH                           I-965                                                                             H       OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O  H    OMe  Me  CH                           I-966                                                                             H       OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O  H    OMe  Me  N                            I-967                                                                             H       OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O  H    OMe  OMe CH                           I-968                                                                             H       OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  Me  CH                           I-969                                                                             H       OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  Me  N                            I-970                                                                             H       OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  OMe CH                           I-971                                                                             H       OCH.sub.2 CH.sub.2 OBu                                                                   H        O  H    OMe  OMe N                            I-972                                                                             H       OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  Me  CH                           I-973                                                                             H       OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  Me  N                            I-974                                                                             H       OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  OMe CH                           I-975                                                                             H       OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O  H    OMe  OMe N                            I-976                                                                             H       OCH.sub.2 CH.sub.2 OEt                                                                   H        O  H    OMe  Me  CH                           I-977                                                                             H       OCH.sub.2 CH.sub.2 OEt                                                                   H        O  H    OMe  Me  N                            I-978                                                                             H       OCH.sub.2 CH.sub.2 OEt                                                                   H        O  H    OMe  OMe CH                           I-979                                                                             H       OCH.sub.2 CH.sub.2 OMe                                                                   H        O  H    OMe  Me  CH                           I-980                                                                             H       OCH.sub.2 CH.sub.2 OMe                                                                   H        O  H    OMe  OMe CH                           I-981                                                                             H       OCH.sub.2 CH.sub.2 OPh                                                                   H        O  H    OMe  OMe CH                           I-982                                                                             H       OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O  H    OMe  Me  CH                           I-983                                                                             H       OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O  H    OMe  Me  N                            I-984                                                                             H       OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O  H    OMe  OMe CH                           I-985                                                                             H       OCH.sub.2 CH.sub.2 SMe                                                                   H        O  H    Me   OMe CH                           I-986                                                                             H       OCH.sub.2 CH.sub.2 SMe                                                                   H        O  H    Me   OMe N                            I-987                                                                             H       OCH.sub.2 CH.sub.2 SMe                                                                   H        O  H    OMe  OMe CH                           I-988                                                                             H       OCH.sub.2 CHCl.sub.2                                                                     H        O  H    Me   OMe CH                           I-989                                                                             H       OCH.sub.2 CHCl.sub.2                                                                     H        O  H    Me   OMe N                            I-990                                                                             H       OCH.sub.2 CHCl.sub.2                                                                     H        O  H    OMe  OMe CH                           I-991                                                                             H       OCH.sub.2 CHF.sub.2                                                                      H        O  H    Me   OMe CH                           I-992                                                                             H       OCH.sub.2 CHF.sub.2                                                                      H        O  H    Me   OMe N                            I-993                                                                             H       OCH.sub.2 CHF.sub.2                                                                      H        O  H    OMe  OMe CH                           I-994                                                                             H       OCH.sub.2 CN                                                                             H        O  H    Me   OMe CH                           I-995                                                                             H       OCH.sub.2 CN                                                                             H        O  H    Me   OMe N                            I-996                                                                             H       OCH.sub.2 CN                                                                             H        O  H    OMe  OMe CH                           I-997                                                                             H       OCH.sub.2 COOEt                                                                          H        O  H    OMe  OMe CH                           I-998                                                                             H       OCH.sub.2 COOMe                                                                          H        O  H    Me   OMe CH                           I-999                                                                             H       OCH.sub.2 COOMe                                                                          H        O  H    Me   OMe N                            I-1000                                                                            H       OCH.sub.2 COOMe                                                                          H        O  H    OMe  OMe CH                           I-1001                                                                            H       OCH.sub.2 COOPr                                                                          H        O  H    Me   OMe CH                           I-1002                                                                            H       OCH.sub.2 COOPr                                                                          H        O  H    Me   OMe N                            I-1003                                                                            H       OCH.sub.2 COOPr                                                                          H        O  H    OMe  OMe CH                           I-1004                                                                            H       OCH.sub.2 COOPr-i                                                                        H        O  H    Me   OMe CH                           I-1005                                                                            H       OCH.sub.2 COOPr-i                                                                        H        O  H    Me   OMe N                            I-1006                                                                            H       OCH.sub.2 COOPr-i                                                                        H        O  H    OMe  OMe CH                           I-1007                                                                            H       OCH.sub.2 OBn                                                                            H        O  H    Me   OMe CH                           I-1008                                                                            H       OCH.sub.2 OBn                                                                            H        O  H    Me   OMe N                            I-1009                                                                            H       OCH.sub.2 OBn                                                                            H        O  H    OMe  OMe CH                           I-1010                                                                            H       OCH.sub.2 OBu-t                                                                          H        O  H    Me   OMe CH                           I-1001                                                                            H       OCH.sub.2 OBu-t                                                                          H        O  H    Me   OMe N                            I-1012                                                                            H       OCH.sub.2 OBu-t                                                                          H        O  H    OMe  OMe CH                           I-1013                                                                            H       OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O  H    Me   OMe CH                           I-1014                                                                            H       OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O  H    Me   OMe N                            I-1015                                                                            H       OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O  H    OMe  OMe CH                           I-1016                                                                            H       OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O  H    Me   OMe CH                           I-1017                                                                            H       OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O  H    Me   OMe N                            I-1018                                                                            H       OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O  H    OMe  OMe CH                           I-1019                                                                            H       OCH.sub.2 OEt                                                                            H        O  H    Me   OMe CH                           I-1020                                                                            H       OCH.sub.2 OEt                                                                            H        O  H    Me   OMe N                            I-1021                                                                            H       OCH.sub.2 OEt                                                                            H        O  H    OMe  OMe CH                           I-1022                                                                            H       OCH.sub.2 OMe                                                                            H        O  H    Me   OMe CH                           I-1023                                                                            H       OCH.sub.2 OMe                                                                            H        O  H    Me   OMe N                            I-1024                                                                            H       OCH.sub.2 OMe                                                                            H        O  H    OMe  OMe CH                           I-1025                                                                            H       OCH.sub.2 SMe                                                                            H        O  H    Me   OMe CH                           I-1026                                                                            H       OCH.sub.2 SMe                                                                            H        O  H    Me   OMe N                            I-1027                                                                            H       OCH.sub.2 SMe                                                                            H        O  H    OMe  OMe CH                           I-1028                                                                            H       OCHF.sub.2 H        O  H    Me   OMe CH                           I-1029                                                                            H       OCHF.sub.2 H        O  H    Me   OMe N                            I-1030                                                                            H       OCHF2      H        O  H    OMe  OMe CH                           I-1031                                                                            H       OCOEt      H        O  H    Me   OMe CH                           I-1032                                                                            H       OCOEt      H        O  H    Me   OMe N                            I-1033                                                                            H       OCOEt      H        O  H    OMe  OMe CH                           I-1034                                                                            H       OCOMe      H        O  H    OMe  OMe CH                           I-1035                                                                            H       OCONMe.sub.2                                                                             H        O  H    Me   OMe CH                           I-1036                                                                            H       OCONMe.sub.2                                                                             H        O  H    Me   OMe N                            I-1037                                                                            H       OCONMe.sub.2                                                                             H        O  H    OMe  OMe CH                           I-1038                                                                            H       OCOPh      H        O  H    Me   OMe CH                           I-1039                                                                            H       OCOPh      H        O  H    Me   OMe N                            I-1040                                                                            H       OCOPh      H        O  H    OMe  OMe CH                           I-1041                                                                            H       OCOPr      H        O  H    Me   OMe CH                           I-1042                                                                            H       OCOPr      H        O  H    Me   OMe N                            I-1043                                                                            H       OCOPr      H        O  H    OMe  OMe CH                           I-1044                                                                            H       OEt        H        O  H    Me   Me  CH                           I-1045                                                                            H       OEt        H        O  H    OMe  Me  CH                           I-1046                                                                            H       OEt        H        O  H    OMe  Me  N                            I-1047                                                                            H       OEt        H        O  H    OMe  OMe CH                           I-1048                                                                            H       OH         H        O  H    OMe  OMe CH                           I-1049                                                                            H       OMe        5-Cl     O  H    OMe  Me  N                            I-1050                                                                            H       OMe        5-Cl     O  H    OMe  OMe CH                           I-1051                                                                            H       OMe        5-OMe    O  H    OMe  Me  CH                           I-1052                                                                            H       OMe        H        O  H    Cl   OMe CH                           I-1053                                                                            H       OMe        H        O  H    OMe  Me  CH                           I-1054                                                                            H       OMe        H        O  H    OMe  OMe N                            I-1055                                                                            H       OMe        H        O  H    Me   Me  CH                           I-1056                                                                            H       OMe        H        O  H    OMe  Me  N                            I-1057                                                                            H       OMe        H        O  H    OMe  OMe CH                           I-1058                                                                            H       OPh        H        O  H    OMe  OMe CH                           I-1059                                                                            H       OPh(2-Me)  H        O  H    OMe  OMe CH                           I-1060                                                                            H       OPh(3-OMe) H        O  H    OMe  OMe CH                           I-1061                                                                            H       OPh(4-Cl)  H        O  H    OMe  OMe CH                           I-1062                                                                            H       OPr        H        O  H    Cl   OMe CH                           I-1063                                                                            H       OPr        H        O  H    Me   Me  CH                           I-1064                                                                            H       OPr        H        O  H    OMe  Me  CH                           I-1065                                                                            H       OPr        H        O  H    OMe  Me  N                            I-1066                                                                            H       OPr        H        O  H    OMe  OMe CH                           I-1067                                                                            H       OPr-i      H        O  H    Me   Me  CH                           I-1068                                                                            H       OPr-i      H        O  H    OMe  Me  CH                           I-1069                                                                            H       OPr-i      H        O  H    OMe  Me  N                            I-1070                                                                            H       OPr-i      H        O  H    OMe  OMe CH                           I-1071                                                                            H       Ph         H        O  H    OMe  OMe CH                           I-1072                                                                            H       Pr         H        O  H    Me   OMe CH                           I-1073                                                                            H       Pr         H        O  H    Me   OMe N                            I-1074                                                                            H       Pr         H        O  H    OMe  OMe CH                           I-1075                                                                            H       Pr-i       H        O  H    Me   OMe CH                           I-1076                                                                            H       Pr-i       H        O  H    Me   OMe N                            I-1077                                                                            H       Pr-i       H        O  H    OMe  OMe CH                           I-1078                                                                            H       SBu        H        O  H    Cl   OMe CH                           I-1079                                                                            H       SBu        H        O  H    OMe  OMe CH                           I-1080                                                                            H       SCF.sub.3  H        O  H    Me   OMe CH                           I-1081                                                                            H       SCF.sub.3  H        O  H    Me   OMe N                            I-1082                                                                            H       SCF.sub.3  H        O  H    OMe  OMe CH                           I-1083                                                                            H       SCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe CH                           I-1084                                                                            H       SCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    Me   OMe N                            I-1085                                                                            H       SCH.sub.2 CH.sub.2 Cl                                                                    H        O  H    OMe  OMe CH                           I-1086                                                                            H       SCH.sub.2 CH.sub.2 F                                                                     H        O  H    Me   OMe CH                           I-1087                                                                            H       SCH.sub.2 CH.sub.2 F                                                                     H        O  H    Me   OMe N                            I-1088                                                                            H       SCH.sub.2 CH.sub.2 F                                                                     H        O  H    OMe  OMe CH                           I-1089                                                                            H       SEt        H        O  H    OMe  Me  N                            I-1090                                                                            H       SEt        H        O  H    OMe  OMe CH                           I-1091                                                                            H       SH         H        O  H    OMe  OMe CH                           I-1092                                                                            H       SMe        H        O  H    OMe  OMe CH                           I-1093                                                                            H       SO.sub.2 Bu                                                                              H        O  H    OMe  OMe CH                           I-1094                                                                            H       SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    Me   OMe CH                           I-1095                                                                            H       SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    Me   OMe N                            I-1096                                                                            H       SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O  H    OMe  OMe CH                           I-1097                                                                            H       SO.sub.2 Et                                                                              H        O  H    OMe  OMe CH                           I-1098                                                                            H       SO.sub.2 Me                                                                              H        O  H    OMe  OMe CH                           I-1099                                                                            H       SO.sub.2 NMe.sub.2                                                                       H        O  H    OMe  OMe CH                           I-1100                                                                            H       SO.sub.2 NEt.sub.2                                                                       H        O  H    Me   OMe CH                           I-1101                                                                            H       SO.sub.2 NEt.sub.2                                                                       H        O  H    Me   OMe N                            I-1102                                                                            H       SO.sub.2 NEt.sub.2                                                                       H        O  H    OMe  OMe CH                           I-1103                                                                            H       SO.sub.2 NH.sub.2                                                                        H        O  H    OMe  OMe CH                           I-1104                                                                            H       SO.sub.2 NHBn                                                                            H        O  H    OMe  OMe CH                           I-1105                                                                            H       SO.sub.2 NHCH.sub.2 CCH                                                                  H        O  H    OMe  OMe CH                           I-1106                                                                            H       SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                           H        O  H    OMe  OMe CH                           I-1007                                                                            H       SO.sub.2 NHMe                                                                            H        O  H    OMe  OMe CH                           I-1008                                                                            H       SO.sub.2 NHOEt                                                                           H        O  H    Me   OMe CH                           I-1009                                                                            H       SO.sub.2 NHOEt                                                                           H        O  H    Me   OMe N                            I-1110                                                                            H       SO.sub.2 NHOEt                                                                           H        O  H    OMe  OMe CH                           I-1111                                                                            H       SO.sub.2 NHOMe                                                                           H        O  H    OMe  OMe CH                           I-1112                                                                            H       SO.sub.2 NHPh                                                                            H        O  H    OMe  OMe CH                           I-1113                                                                            H       SO.sub.2 Pr                                                                              H        O  H    OMe  OMe CH                           I-1114                                                                            H       SO.sub.2 Pr-i                                                                            H        O  H    Cl   OMe CH                           I-1115                                                                            H       SO.sub.2 Pr-i                                                                            H        O  H    OMe  OMe CH                           I-1116                                                                            H       SOEt       H        O  H    Me   OMe CH                           I-1117                                                                            H       SOEt       H        O  H    Me   OMe N                            I-1118                                                                            H       SOEt       H        O  H    OMe  OMe CH                           I-1119                                                                            H       SOMe       H        O  H    OMe  OMe CH                           I-1120                                                                            H       SPr        H        O  H    Cl   OMe CH                           I-1121                                                                            H       SPr        H        O  H    OMe  Me  CH                           I-1122                                                                            H       SPr        H        O  H    OMe  Me  N                            I-1123                                                                            H       SPr        H        O  H    OMe  OMe CH                           I-1124                                                                            H       SPr-i      H        O  H    Cl   OMe CH                           I-1125                                                                            H       SPr-i      H        O  H    OMe  OMe CH                           I-1126                                                                            H       NO.sub.2   H        O  H    Me   OMe N  182-184                   I-1127                                                                            H       SEt        H        O  H    Cl   OMe CH                           I-1128                                                                            H       SEt        H        O  H    Me   Me  CH                           I-1129                                                                            H       SEt        H        O  H    OMe  OMe N                            I-1130                                                                            H       SBu        H        O  H    OMe  Me  CH                           I-1131                                                                            H       Sbu        H        O  H    OMe  Me  N                            I-1132                                                                            H       SPr-i      H        O  H    OMe  Me  CH                           I-1133                                                                            H       SPr-i      H        O  H    OMe  Me  N                            I-1134                                                                            H       SOEt       H        O  H    OMe  OMe N                            I-1135                                                                            H       SO.sub.2 Et                                                                              H        O  H    OMe  Me  CH                           I-1136                                                                            H       SO.sub.2 Et                                                                              H        O  H    OMe  Me  N                            I-1137                                                                            H       SO.sub.2 Et                                                                              H        O  H    OMe  Cl  CH                           I-1138                                                                            H       SO.sub.2 Pr                                                                              H        O  H    OMe  Me  CH                           I-1139                                                                            H       SO.sub.2 Pr                                                                              H        O  H    OMe  Me  N                            I-1140                                                                            H       SO.sub.2 Pr                                                                              H        O  H    OMe  Cl  CH                           I-1141                                                                            H       SO.sub.2 Bu                                                                              H        O  H    OMe  Me  CH                           I-1142                                                                            H       SO.sub.2 Bu                                                                              H        O  H    OMe  Me  N                            I-1143                                                                            H       SO.sub.2 Bu                                                                              H        O  H    OMe  Cl  CH                           I-1144                                                                            H       SO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  CH                           I-1145                                                                            H       SO.sub.2 Pr-i                                                                            H        O  H    OMe  Me  N                            I-1146                                                                            H       COOPr      H        O  H    OMe  Me  N                            I-1147                                                                            H       NO.sub.2   H        O  H    OMe  Cl  CH                           I-1148                                                                            H       CONMe.sub.2                                                                              H        O  H    OMe  Me  CH                           I-1149                                                                            H       Br         H        O  H    OMe  Cl  CH                           I-1150                                                                            H                                                                                      ##STR29## H        O  H    OMe  OMe CH                           I-1151                                                                            H       OCH.sub.2 -Bu-t                                                                          H        O  H    OMe  OMe CH                           I-1152                                                                            H       OCH.sub.2 -Bu-t                                                                          H        O  H    Me   OMe CH                           I-1153                                                                            H       OCH.sub.2 CHCMe.sub.2                                                                    H        O  H    OMe  OMe CH                           I-1154                                                                            H       OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O  H    OMe  OMe CH                           I-1155                                                                            H       OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O  H    Me   OMe CH                           I-1156                                                                            H       OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O  H    Me   OMe N                            I-1157                                                                            H       CH.sub.2 CH.sub.2 N.sub.3                                                                H        O  H    OMe  OMe CH                           I-1158                                                                            H                                                                                      ##STR30## H        O  H    OMe  OMe CH                           I-1159                                                                            H       COCF.sub.3 H        O  H    OMe  OMe CH                           I-1160                                                                            H       COOCH.sub.2 CHCHCl                                                                       H        O  H    OMe  OMe CH                           I-1161                                                                            H       SO.sub.2 CF.sub.3                                                                        H        O  H    OMe  OMe CH                           I-1162                                                                            H       OCOCF.sub.3                                                                              H        O  H    OMe  OMe CH                           I-1163                                                                            H       OCH.sub.2 OPh                                                                            H        O  H    OMe  OMe CH                           I-1164                                                                            H       CHNOH      H        O  H    OMe  OMe CH                           I-1165                                                                            H       CHNOCH.sub.2 CHCH.sub.2                                                                  H        O  H    OMe  OMe CH                           I-1166                                                                            H       CHNOCH.sub.2 CCH                                                                         H        O  H    OMe  OMe CH                           I-1167                                                                            H       C(Me)NOBn  H        O  H    OMe  OMe CH                           I-1168                                                                            H       C(Me)NOPh  H        O  H    OMe  OMe CH                           I-1169                                                                            H       C(Bn)NOMe  H        O  H    OMe  OMe CH                           I-1170                                                                            H       C(Ph)NOMe  H        O  H    OMe  OMe CH                           I-1171                                                                            H       C(CF.sub.3)NOMe                                                                          H        O  H    OMe  OMe CH                           I-1172                                                                            H       COOCH.sub.2 CH.sub.2 Cl                                                                  H        O  H    OMe  OMe CH                           I-1173                                                                            H       COOCH.sub.2 CF.sub.3                                                                     H        O  H    OMe  OMe CH                           I-1174                                                                            H       Cl         S-Cl     O  H    OMe  Me  N                            I-1175                                                                            H       Cl         5-OMe    O  H    OMe  OMe CH                           I-1176                                                                            H       Cl         5-F      O  H    OMe  OMe CH                           I-1177                                                                            H       F          5-Cl     O  H    OMe  OMe CH                           I-1178                                                                            H       F          5-F      O  H    OMe  OMe CH                           I-1179                                                                            H       COOMe      5-Cl     O  H    OMe  OMe CH                           I-1180                                                                            H       COOEt      5-Cl     O  H    OMe  OMe CH                           I-1181                                                                            H       COOPr      5-Cl     O  H    OMe  OMe CH                           I-1182                                                                            H       COOPr-i    5-Cl     O  H    OMe  OMe CH                           I-1183                                                                            H       OMe        5-COOMe  O  H    OMe  OMe CH                           I-1184                                                                            H       COOMe      5-OMe    O  H    OMe  OMe CH                           I-1185                                                                            H       ONCHMe     H        O  H    OMe  OMe CH                           I-1186                                                                            H       ONCMe.sub.2                                                                              H        O  H    OMe  OMe CH                           I-1187                                                                            H       ONCHBn     H        O  H    OMe  OMe CH                           I-1188                                                                            H       OCH.sub.2 CH.sub.2 F                                                                     H        O  H    OMe  Me  CH                           I-1189                                                                            H       OCH.sub.2 CH.sub.2 F                                                                     H        O  H    OMe  Me  N                            I-1190                                                                            H       H          5-CN     O  H    OMe  OMe CH                           I-1191                                                                            H       H          5-CF.sub.3                                                                             O  H    OMe  OMe CH                           I-1192                                                                            H       H          5-COOMe  O  H    OMe  OMe CH                           I-1193                                                                            H       H          5-COOEt  O  H    OMe  OMe CH                           I-1194                                                                            H       H          5-COOPr  O  H    OMe  OMe CH                           I-1195                                                                            H       H          5-COOPr-i                                                                              O  H    OMe  OMe CH                           I-1196                                                                            H       H          5-COOCH.sub.2 CH.sub.2 Cl                                                              O  H    OMe  OMe CH                           I-1197                                                                            H       H          5-COOCH.sub.2 CH.sub.2 F                                                               O  H    OMe  OMe CH                           I-1198                                                                            H       H          5-COOCH.sub.2 CF.sub.3                                                                 O  H    OMe  OMe CH                           I-1199                                                                            H       H          5-COOCH.sub.2 OMe                                                                      O  H    OMe  OMe CH                           I-1200                                                                            H       H          5-CONMe.sub.2                                                                          O  H    OMe  OMe CH                           I-1201                                                                            H       H          5-OCH.sub.2 CH.sub.2 F                                                                 O  H    OMe  OMe CH                           I-1202                                                                            H       H          5-OCHF.sub.2                                                                           O  H    OMe  OMe CH                           I-1203                                                                            H       H          5-OCH.sub.2 CF.sub.3                                                                   O  H    OMe  OMe CH                           I-1204                                                                            H       H          5-OCH.sub.2 CH.sub.2 CH.sub.2 F                                                        O  H    OMe  OMe CH                           I-1205                                                                            H       H          5-OCH.sub.2 CHCH.sub.2                                                                 O  H    OMe  OMe CH                           I-1206                                                                            H       H          5-OCH.sub.2 CCH                                                                        O  H    OMe  OMe CH                           I-1207                                                                            H       H          5-NO.sub.2                                                                             O  H    OMe  OMe CH                           I-1208                                                                            H       H          5-SMe    O  H    OMe  OMe CH                           I-1209                                                                            H       H          5-SEt    O  H    OMe  OMe CH                           I-1210                                                                            H       H          5-SPr    O  H    OMe  OMe CH                           I-1211                                                                            H       H          5-SPr-i  O  H    OMe  OMe CH                           I-1212                                                                            H       H          5-SO.sub.2 Et                                                                          O  H    OMe  OMe CH                           I-1213                                                                            H       H          5-SO.sub.2 Pr                                                                          O  H    OMe  OMe CH                           I-1214                                                                            H       H          5-SO.sub.2 Pr-i                                                                        O  H    OMe  OMe CH                           I-1215                                                                            H       H          5-SOEt   O  H    OMe  OMe CH                           I-1216                                                                            H       H          5-Me     O  H    OMe  OMe CH                           I-1217                                                                            H       H          5-Et     O  H    OMe  OMe CH                           I-1218                                                                            H       H          5-Pr     O  H    OMe  OMe CH                           I-1219                                                                            H       H          5-SO.sub.2 NMe.sub.2                                                                   O  H    OMe  OMe CH                           I-1220                                                                            H       H          5-OCF.sub.3                                                                            O  H    OMe  OMe CH                           I-1221                                                                            H       H          5-CH.sub.2 CF.sub.3                                                                    O  H    OMe  OMe CH                           I-1222                                                                            H       H          5-CH.sub.2 CHCH.sub.2                                                                  O  H    OMe  OMe CH                           I-1223                                                                            H       H          5-COOMe  O  H    OMe  Me  CH                           I-1224                                                                            H       H          5-COOMe  O  H    OMe  Me  N                            I-1225                                                                            H       H          5-COOMe  O  H    OMe  OMe N                            I-1226                                                                            H       Cl         H        O  CH.sub.3 OCH.sub.2                                                                 OMe  OMe CH                           I-1227                                                                            H       Cl         H        O  H    OMe  NMe.sub.2                                                                         N                            I-1228                                                                            H       Cl         H        O  H    OMe  NHMe                                                                              N                            I-1229                                                                            H                                                                                      ##STR31## H        O  H    Me   OMe CH                           I-1230                                                                            H                                                                                      ##STR32## H        O  H    Me   OMe N                            I-1231                                                                            H                                                                                      ##STR33## H        O  H    OMe  OMe CH                           I-1232                                                                            H                                                                                      ##STR34## H        O  H    OMe  OMe CH                           I-1233                                                                            H                                                                                      ##STR35## H        O  H    Me   OMe CH                           I-1234                                                                            H                                                                                      ##STR36## H        O  H    Me   OMe N                            I-1235                                                                            H                                                                                      ##STR37## H        O  H    OMe  OMe CH                           I-1236                                                                            H                                                                                      ##STR38## H        O  H    Me   OMe CH                           I-1237                                                                            H                                                                                      ##STR39## H        O  H    Me   OMe N                            I-1238                                                                            H                                                                                      ##STR40## H        O  H    OMe  OMe CH                           I-1239                                                                            H                                                                                      ##STR41## H        O  H    Me   OMe CH                           I-1240                                                                            H                                                                                      ##STR42## H        O  H    Me   OMe N                            I-1241                                                                            H       OC.sub.2 H.sub.4O*  O  H    OMe  OMe CH                           I-1242                                                                            H       OC.sub.2 H.sub.4O*  O  H    Me   OMe CH                           I-1243                                                                            H       OC.sub.2 H.sub.4O*  O  H    Me   OMe N                            I-1244                                                                            H       SC.sub.2 H.sub.4S*  O  H    OMe  OMe CH                           I-1245                                                                            H       SC.sub.2 H.sub.4S*  O  H    Me   OMe CH                           I-1246                                                                            H       SC.sub.2 H.sub.4S*  O  H    Me   OMe N                            I-1247                                                                            H       OCH.sub.2O*         O  H    OMe  OMe CH                           __________________________________________________________________________     *R.sup.3 represents the 5position.                                       

                                      TABLE 2                                     __________________________________________________________________________     ##STR43##                                                                    Comp.                                                                         No. R.sup.1                                                                              R.sup.2    R.sup.3  X Y    A   B    Z mp.(°C.)              __________________________________________________________________________    II-1                                                                              Me     Ph         H        O H    OMe OMe  CH                             II-2                                                                              Me     Bn         H        O H    OMe OMe  CH                             II-3                                                                              Me     SH         H        O H    OMe OMe  CH                             II-4                                                                              Me     SMe        H        O H    OMe OMe  CH                             II-5                                                                              Me     SEt        H        O H    OMe OMe  CH                                                                              156-157                      II-6                                                                              Me     SPr        H        O H    OMe OMe  CH                                                                              143-145                      II-7                                                                              Me     SO.sub.2 Me                                                                              H        O H    OMe OMe  CH                             II-8                                                                              Me     SO.sub.2 Et                                                                              H        O H    OMe OMe  CH                                                                              196-198                      II-9                                                                              Me     SOMe       H        O H    OMe OMe  CH                             II-10                                                                             Me     SO.sub.2 NHMe                                                                            H        O H    OMe OMe  CH                             II-11                                                                             Me     SO.sub.2 NHOMe                                                                           H        O H    OMe OMe  CH                             II-12                                                                             Me     SO.sub.2 NMe.sub.2                                                                       H        O H    OMe OMe  CH                                                                              169-171                      II-13                                                                             Me     SO.sub.2 NHBn                                                                            H        O H    OMe OMe  CH                             II-14                                                                             Me     SO.sub.2 NHPh                                                                            H        O H    OMe OMe  CH                             II-15                                                                             Me     SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                           H        O H    OMe OMe  CH                             II-16                                                                             Me     SO.sub.2 NHCH.sub.2 C CH                                                                 H        O H    OMe OMe  CH                             II-17                                                                             H      Cl         H        O H    OMe OMe  CH                                                                              191-193                      II-18                                                                             Me     Cl         H        O H    Me  Me   CH                                                                              210-213                      II-19                                                                             Me     Cl         5-Cl     O H    OMe OMe  CH                                                                              203-205                      II-20                                                                             Et     Cl         H        O H    OMe OMe  CH                                                                              174-175                      II-21                                                                             Ph     Cl         H        O H    OMe OMe  CH                                                                              221-223                      II-22                                                                             Bn     Cl         H        O H    OMe OMe  CH                             II-23                                                                             Me     H          H        O H    OMe OMe  CH                                                                              199-202                      II-24                                                                             Me     H          H        O H    Me  Me   CH                                                                              208-210                      II-25                                                                             Me     H          H        O H    OMe Me   N 172-174                      II-26                                                                             Me     F          H        O H    OMe OMe  CH                                                                              205-206                      II-27                                                                             Me     Br         H        O H    OMe OMe  CH                                                                              179-182                      II-28                                                                             Me     Me         H        O H    OMe OMe  CH                                                                              178-180                      II-29                                                                             Me     CN         H        O H    OMe OMe  CH                                                                              189-191                      II-30                                                                             Me     CF.sub.3   H        O H    OMe OMe  CH                             II-31                                                                             Me     Cl         H        O H    OMe Me   CH                                                                              202-204                      II-32                                                                             Me     Cl         H        O H    OMe Me   N 170-172                      II-33                                                                             Me     F          H        O H    Me  Me   CH                                                                              207-209                      II-34                                                                             Me     F          H        O H    OMe Me   N 178-180                      II-35                                                                             Me     F          H        O H    OMe Me   CH                                                                              185-187                      II-36                                                                             Me     H          5-Cl     O H    OMe OMe  CH                                                                              215-216                      II-37                                                                             Me     H          5-Cl     O H    Me  Me   CH                                                                              192-194                      II-38                                                                             Me     H          5-Cl     O H    OMe Me   N 176-178                      II-39                                                                             Me     H          6-Cl     O H    OMe OMe  CH                                                                              210-212                      II-40                                                                             Me     H          6-Cl     O H    Me  Me   CH                                                                              217-220                      II-41                                                                             Me     H          6-Cl     O H    OMe Me   N 181-183                      II-42                                                                             Me     H          7-Cl     O H    OMe OMe  CH                                                                              223-225                      II-43                                                                             Me     H          7-Cl     O H    OMe Me   N 167-169                      II-44                                                                             Me     Cl         H        S H    OMe OMe  CH                             II-45                                                                             Me     Cl         H        O Me   OMe OMe  CH                             II-46                                                                             Me     COH        H        O H    OMe OMe  CH                             II-47                                                                             Me     COMe       H        O H    OMe OMe  CH                             II-48                                                                             Me     COEt       H        O H    OMe OMe  CH                             II-49                                                                             Me     COPh       H        O H    OMe OMe  CH                             II-50                                                                             Me     COCH.sub.2 CHCH.sub.2                                                                    H        O H    OMe OMe  CH                             II-51                                                                             Me     COCH.sub.2 C CH                                                                          H        O H    OMe OMe  CH                             II-52                                                                             Me     COBn       H        O H    OMe OMe  CH                             II-53                                                                             Me     NO.sub.2   H        O H    OMe OMe  CH                                                                              155-157                      II-54                                                                             Me     NH.sub.2   H        O H    OMe OMe  CH                             II-55                                                                             Me     NHMe       H        O H    OMe OMe  CH                                                                              143-144                      II-56                                                                             Me     NMe.sub.2  H        O H    OMe OMe  CH                                                                              183-185                      II-57                                                                             Me     NHCOMe     H        O H    OMe OMe  CH                             II-58                                                                             Me     NHCOPh     H        O H    OMe OMe  CH                             II-59                                                                             Me     NHCOCH.sub.2 Cl                                                                          H        O H    OMe OMe  CH                             II-60                                                                             Me     NHSO.sub.2 CH.sub.3                                                                      H        O H    OMe OMe  CH                             II-61                                                                             Me     NHSO.sub.2 Ph                                                                            H        O H    OMe OMe  CH                             II-62                                                                             Me     CO.sub.2 H H        O H    OMe OMe  CH                             II-63                                                                             Me     CO.sub.2 Me                                                                              H        O H    OMe OMe  CH                                                                              179-181                      II-64                                                                             Me     CO.sub.2 Et                                                                              H        O H    OMe OMe  CH                                                                              181-182                      II-65                                                                             Me     CO.sub.2 Pr                                                                              H        O H    OMe OMe  CH                                                                              188-190                      II-66                                                                             Me     CO.sub.2 Pr-i                                                                            H        O H    OMe OMe  CH                                                                              200-202                      II-67                                                                             Me     CO.sub.2 Bu                                                                              H        O H    OMe OMe  CH                                                                              189-190                      II-68                                                                             Me     CO.sub.2 Pen                                                                             H        O H    OMe OMe  CH                             II-69                                                                             Me     CO.sub.2 Bn                                                                              H        O H    OMe OMe  CH                             II-70                                                                             Me     CO.sub.2 Ph                                                                              H        O H    OMe OMe  CH                             II-71                                                                             Me     CO.sub.2 CH.sub.2 CH.sub.2 F                                                             H        O H    OMe OMe  CH                             II-72                                                                             Me     CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O H    OMe OMe  CH                             II-73                                                                             Me     CO.sub.2 CH.sub.2 C CH                                                                   H        O H    OMe OMe  CH                             II-74                                                                             Me     CO.sub.2 Me                                                                              H        O H    OCHF.sub.2                                                                        OCHF.sub.2                                                                         CH                             II-75                                                                             Me     CO.sub.2 Et                                                                              H        O H    OCHF.sub.2                                                                        OCHF.sub.2                                                                         CH                             II-76                                                                             Me     CO.sub.2 Me                                                                              H        O H    OMe Cl   CH                             II-77                                                                             Me     CO.sub.2 Me                                                                              H        O H    OMe Me   CH                             II-78                                                                             Me     CO.sub.2 Me                                                                              H        O H    OMe Me   N                              II-79                                                                             Me     CO.sub.2 Et                                                                              H        O H    OMe Me   N                              II-80                                                                             Me     CO.sub.2 Me                                                                              H        O H    OMe OCHF.sub.2                                                                         CH                             II-81                                                                             Me     CO.sub.2 Me                                                                              5-F      O H    OMe OMe  CH                             II-82                                                                             Et     CO.sub.2 Me                                                                              H        O H    OMe OMe  CH                                                                              147-148                      II-83                                                                             Bu     CO.sub.2 Me                                                                              H        O H    OMe OMe  CH                             II-84                                                                             Bn     CO.sub.2 Me                                                                              H        O H    OMe OMe  CH                             II-85                                                                             Ph     CO.sub.2 Me                                                                              H        O H    OMe OMe  CH                             II-86                                                                             H      CO.sub.2 Et                                                                              H        O H    OMe OMe  CH                             II-87                                                                             Me     CO.sub.2 Me                                                                              H        S H    OMe OMe  CH                             II-88                                                                             Me     CO.sub.2 Et                                                                              H        S H    OMe OMe  CH                             II-89                                                                             Me     CO.sub.2 Me                                                                              H        O Me   OMe OMe  CH                             II-90                                                                             Me     OH         H        O H    OMe OMe  CH                                                                              179-181                      II-91                                                                             Me     OMe        H        O H    OMe OMe  CH                                                                              162-165                      II-92                                                                             Me     OEt        H        O H    OMe OMe  CH                                                                              153-154                      1I-93                                                                             Me     OPr        H        O H    OMe OMe  CH                                                                              119-120                      II-94                                                                             Me     OPr-i      H        O H    OMe OMe  CH                                                                              176-179                      II-95                                                                             Me     OBu        H        O H    OMe OMe  CH                                                                              184-186                      II-96                                                                             Me     OBn        H        O H    OMe OMe  CH                                                                              200-203                      II-97                                                                             Me     OBn(4-Cl)  H        O H    OMe OMe  CH                             II-98                                                                             Me     OBn(3-OMe) H        O H    OMe OMe  CH                             II-99                                                                             Me     OBn(2-Me)  H        O H    OMe OMe  CH                             II-100                                                                            Me     OPh        H        O H    OMe OMe  CH                             II-101                                                                            Me     OPh(4-Cl)  H        O H    OMe OMe  CH                             II-102                                                                            Me     OPh(3-OMe) H        O H    OMe OMe  CH                             II-103                                                                            Me     OPh(2-Me)  H        O H    OMe OMe  CH                             II-104                                                                            Me     OCH.sub.2 CHCH.sub.2                                                                     H        O H    OMe OMe  CH                                                                              133-136                      II-105                                                                            Me     OCH.sub.2 C CH                                                                           H        O H    OMe OMe  CH                                                                              182-183                      II-106                                                                            Me     OCH.sub.2 CF.sub.3                                                                       H        O H    OMe OMe  CH                                                                              165-170                      II-107                                                                            Me     OCH.sub.2 CH.sub.2 OMe                                                                   H        O H    OMe OMe  CH                                                                              139-141                      II-108                                                                            Me     OCH.sub.2 CH.sub.2 OPh                                                                   H        O H    OMe OMe  CH                             II-109                                                                            Me     OCOMe      H        O H    OMe OMe  CH                             II-110                                                                            Me     OMe        H        O H    OMe Me   CH                                                                              206-208                      II-111                                                                            Me     OMe        H        O H    OMe Me   N 198-201                      II-112                                                                            Me     OMe        H        O H    Me  Me   CH                                                                              193-196                      II-113                                                                            Me     OEt        H        O H    OMe Me   N 179-181                      II-114                                                                            Me     OEt        H        O H    OMe Me   CH                                                                              174-175                      II-115                                                                            Me     OEt        H        O H    Me  Me   CH                                                                              182-183                      II-116                                                                            Me     CONH.sub.2 H        O H    OMe OMe  CH                             II-117                                                                            Me     CONHMe     H        O H    OMe OMe  CH                             II-118                                                                            Me     CONHEt     H        O H    OMe OMe  CH                             II-119                                                                            Me     CONHPr     H        O H    OMe OMe  CH                             II-120                                                                            Me     CONMe.sub.2                                                                              H        O H    OMe OMe  CH                                                                              150-151                      II-121                                                                            Me     CONEt.sub.2                                                                              H        O H    OMe OMe  CH                             II-122                                                                            Me     CONHBn     H        O H    OMe OMe  CH                             II-123                                                                            Me     CONHPh     H        O H    OMe OMe  CH                             II-124                                                                            Me     CONHCH.sub.2 CHCH.sub.2                                                                  H        O H    OMe OMe  CH                             II-125                                                                            Me     CONHCH.sub.2 C CH                                                                        H        O H    OMe OMe  CH                             II-126                                                                            Me     CONHOMe    H        O H    OMe OMe  CH                             II-127                                                                            Me     H          5-F      O H    OMe OMe  CH                                                                              205-208                      II-128                                                                            Me     H          5-F      O H    Me  Me   CH                                                                              203-206                      II-129                                                                            Me     H          5-F      O H    OMe Me   CH                                                                              186-189                      II-130                                                                            Me     H          5-F      O H    OMe Me   N 175-179                      II-131                                                                            H      COOMe      H        O H    OMe OMe  CH                                                                              179-180                      II-132                                                                            H      COOMe      H        O H    OMe Cl   CH                                                                              193-194                      II-133                                                                            H      Cl         H        O H    OMe Cl   CH                                                                              178-181                      II-134                                                                            Me     Cl         H        O H    OMe OMe  CH                                                                              171-172                      II-135                                                                            Me     SO.sub.2 NH.sub.2                                                                        H        O H    OMe OMe  CH                             II-136                                                                            H      Br         H        O H    OMe OMe  CH                                                                              190-193                      II-137                                                                            Me     H          5-OMe    O H    OMe OMe  CH                                                                              178-181                      II-138                                                                            Me     H          5-OEt    O H    OMe OMe  CH                                                                              188-189                      II-139                                                                            Me     H          5-OPr    O H    OMe OMe  CH                                                                              197-198                      II-140                                                                            Me     OCH(CF.sub.3)Me                                                                          H        O H    OMe OMe  CH                                                                              129-130                      II-141                                                                            Me     OCH.sub.2 CH.sub.2 Cl                                                                    H        O H    OMe OMe  CH                                                                              182-186                      II-142                                                                            Me     OCH.sub.2 CH.sub.2 F                                                                     H        O H    OMe OMe  CH                                                                              162-165                      II-143                                                                            Me     OCH.sub.2 CH.sub.2 OEt                                                                   H        O H    OMe OMe  CH                                                                              138-139                      II-144                                                                            Me     OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O H    OMe OMe  CH                                                                              185-187                      II-145                                                                            Me     OCH.sub.2 CH.sub.2 OBu                                                                   H        O H    OMe OMe  CH                                                                              120-121                      II-146                                                                            Me     OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O H    OMe OMe  CH                                                                              169-171                      II-147                                                                            Me     OCH.sub.2 COOEt                                                                          H        O H    OMe OMe  CH                                                                              163-165                      II-148                                                                            Me     OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O H    OMe OMe  CH                                                                              126-129                      II-149                                                                            Me     SBu        H        O H    OMe OMe  CH                                                                              156-158                      II-150                                                                            Me     SPr-i      H        O H    OMe OMe  CH                                                                              183-184                      II-151                                                                            Me     SO.sub.2 Pr                                                                              H        O H    OMe OMe  CH                                                                              202-204                      II-152                                                                            Me     SO.sub.2 Bu                                                                              H        O H    OMe OMe  CH                                                                              201-203                      II-153                                                                            Me     SO.sub.2 Pr-i                                                                            H        O H    OMe OMe  CH                                                                              185-187                      II-154                                                                            Me     NHBn       H        O H    OMe OMe  CH                                                                              167-168                      II-155                                                                            Me     NEt.sub.2  H        O H    OMe OMe  CH                                                                              173-175                      II-156                                                                            Me     OMe        5-Cl     O H    OMe OMe  CH                                                                              211-212                      II-157                                                                            Me     Br         H        O H    OMe Me   CH                                                                              187-189                      II-158                                                                            Et     Cl         H        O H    OMe Me   CH                                                                              205-206                      II-159                                                                            Ph     Cl         H        O H    OMe Me   CH                                                                              215-217                      II-160                                                                            Me     OPr        H        O H    OMe Me   CH                                                                              174-175                      II-161                                                                            Me     OBu        H        O H    OMe Me   CH                                                                              169-171                      II-162                                                                            Me     OPr-i      H        O H    OMe Me   CH                                                                              157-159                      II-163                                                                            Me     H          5-OMe    O H    OMe Me   CH                                                                              206-208                      II-164                                                                            Me     H          5-OEt    O H    OMe Me   CH                                                                              174-176                      II-165                                                                            Me     H          5-OPr    O H    OMe Me   CH                                                                              176-178                      II-166                                                                            Me     OCH.sub.2 CF.sub.3                                                                       H        O H    OMe Me   CH                                                                              150-153                      II-167                                                                            Me     OCH(CF.sub.3)Me                                                                          H        O H    OMe Me   CH                                                                              112-114                      II-168                                                                            Me     OCH.sub.2 CH.sub.2 OMe                                                                   H        O H    OMe Me   CH                                                                              138-139                      II-169                                                                            Me     OCH.sub.2 CH.sub.2 OEt                                                                   H        O H    OMe Me   CH                                                                              160-163                      II-170                                                                            Me     OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O H    OMe Me   CH                                                                              130-132                      II-171                                                                            Me     OCH.sub.2 CH.sub.2 OBu                                                                   H        O H    OMe Me   CH                                                                              104-106                      II-172                                                                            Me     OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O H    OMe Me   CH                                                                              148-149                      II-173                                                                            Me     OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O H    OMe Me   CH                                                                              126-129                      II-174                                                                            Me     SPr        H        O H    OMe Me   CH                                                                              164-165                      II-175                                                                            Me     CO.sub.2 Pr                                                                              H        O H    OMe Me   CH                                                                              179-181                      II-176                                                                            Me     CO.sub.2 Pr-i                                                                            H        O H    OMe Me   CH                                                                              187-190                      II-177                                                                            Me     CO.sub.2 Bu                                                                              H        O H    OMe Me   CH                                                                              189-192                      II-178                                                                            Me     NO.sub.2   H        O H    OMe Me   CH                                                                              161-163                      II-179                                                                            Me     CN         H        O H    OMe Me   CH                                                                              195-197                      II-180                                                                            Me     Br         H        O H    OMe Me   N 172-174                      II-181                                                                            Et     Cl         H        O H    OMe Me   N 192-194                      II-182                                                                            Me     OPr        H        O H    OMe Me   N 176-177                      II-183                                                                            Me     OBu        H        O H    OMe Me   N 143-145                      II-184                                                                            Me     OPr-i      H        O H    OMe Me   N 155-156                      II-185                                                                            Me     H          5-OMe    O H    OMe Me   N 171-174                      II-186                                                                            Me     H          5-OEt    O H    OMe Me   N 180-182                      II-187                                                                            Me     H          5-OPr    O H    OMe Me   N 168-170                      II-188                                                                            Me     OCH.sub.2 CF.sub.3                                                                       H        O H    OMe Me   N 168-170                      II-189                                                                            Me     OCH.sub.2 CH.sub.2 OEt                                                                   H        O H    OMe Me   N 168-170                      II-190                                                                            Me     OCH.sub.2 CH.sub.2 OPr-i                                                                 H        O H    OMe Me   N 153-155                      II-191                                                                            Me     OCH.sub.2 CH.sub.2 OBu                                                                   H        O H    OMe Me   N 121-123                      II-192                                                                            Me     OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O H    OMe Me   N 161-162                      II-193                                                                            Me     OCH.sub.2 CH.sub.2 NMe.sub.2                                                             H        O H    OMe Me   N 119-121                      II-194                                                                            Me     SEt        H        O H    OMe Me   N 160-162                      II-195                                                                            Me     SPr        H        O H    OMe Me   N 129-131                      II-196                                                                            Me     NMe.sub.2  H        O H    OMe Me   N 131-133                      II-197                                                                            Me     CO.sub.2 Pr-i                                                                            H        O H    OMe Me   N 190-191                      II-198                                                                            Me     CO.sub.2 Bu                                                                              H        O H    OMe Me   N 179-181                      II-199                                                                            Me     CN         H        O H    OMe Me   N 196-197                      II-200                                                                            Me     OMe        5-Cl     O H    OMe Me   N 201-203                      II-201                                                                            Me     Cl         H        O H    Cl  OMe  CH                                                                              187-189                      II-202                                                                            Et     Cl         H        O H    Cl  OMe  CH                                                                              206-208                      II-203                                                                            Ph     Cl         H        O H    Cl  OMe  CH                                                                              202-204                      II-204                                                                            Me     OMe        H        O H    Cl  OMe  CH                                                                              220-223                      II-205                                                                            Me     OPr        H        O H    Cl  OMe  CH                                                                              140-141                      II-206                                                                            Me     OBu        H        O H    Cl  OMe  CH                                                                              153-154                      II-207                                                                            Me     H          5-OMe    O H    Cl  OMe  CH                                                                              174-177                      II-208                                                                            Me     OCH.sub.2 CF.sub.3                                                                       H        O H    Cl  OMe  CH                                                                              175-179                      II-209                                                                            Me     SPr        H        O H    Cl  OMe  CH                                                                              165-167                      II-210                                                                            Me     SBu        H        O H    Cl  OMe  CH                                                                              156-157                      II-211                                                                            Me     SPr-i      H        O H    Cl  OMe  CH                                                                              177-179                      II-212                                                                            Me     SO.sub.2 Pr-i                                                                            H        O H    Cl  OMe  CH                                                                              184-186                      II-213                                                                            Me     NHBn       H        O H    Cl  OMe  CH                                                                              160-163                      II-214                                                                            Me     NMe.sub.2  H        O H    Cl  OMe  CH                                                                              197-199                      II-215                                                                            Et     Cl         H        O H    Me  Me   CH                                                                              229-231                      II-216                                                                            Me     OPr        H        O H    Me  Me   CH                                                                              172-173                      II-217                                                                            Me     OBu        H        O H    Me  Me   CH                                                                              148-149                      II-218                                                                            Me     OPr-i      H        O H    Me  Me   CH                                                                              187-190                      II-219                                                                            Me     NMe.sub.2  H        O H    Me  Me   CH                                                                              174-176                      II-220                                                                            Me     OMe        H        O H    OMe OMe  N 193-195                      II-221                                                                            Me     H          5-OEt    O H    OMe OMe  N 169-170                      II-222                                                                            Me     H          5-OPr    O H    OMe OMe  N 168-169                      II-223                                                                            Me     OCH.sub.2 CH.sub.2 OBu                                                                   H        O H    OMe OMe  N 132-133                      II-224                                                                            Me     OCH.sub.2 CH.sub.2 OBu-t                                                                 H        O H    OMe OMe  N 162-163                      II-225                                                                            Me     NHMe       H        O H    OMe Me   CH                                                                              164-165                      II-226                                                                            Me     NHMe       H        O H    OMe Me   N 173-175                      II-227                                                                            Me     OMe        5-Cl     O H    OMe Me   CH                                                                              222-225                      II-228                                                                            Me     OMe        5-OMe    O H    OMe OMe  CH                                                                              168-170                      II-229                                                                            Me     OCHF.sub.2 H        O H    OMe OMe  CH                                                                              179-181                      II-230                                                                            Me     OCHF.sub.2 H        O H    Me  OMe  CH                                                                              195-197                      II-231                                                                            Me     OCHF.sub.2 H        O H    Me  OMe  N 165-167                      II-232                                                                            Me     OCH.sub.2 CHF.sub.2                                                                      H        O H    OMe OMe  CH                                                                              178-180                      II-233                                                                            Me     OCH.sub.2 CHF.sub.2                                                                      H        O H    Me  OMe  CH                                                                              180-182                      II-234                                                                            Me     OCH.sub.2 CHF.sub.2                                                                      H        O H    Me  OMe  N 164-166                      II-235                                                                            Me     OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O H    OMe OMe  CH                             II-236                                                                            Me     OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O H    Me  OMe  CH                             II-237                                                                            Me     OCH.sub.2 CH.sub.2 CF.sub.3                                                              H        O H    Me  OMe  N                              II-238                                                                            Me     OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O H    OMe OMe  CH                             II-239                                                                            Me     OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O H    Me  OMe  CH                             II-240                                                                            Me     OCH(CF.sub.2 CF.sub.3)Me                                                                 H        O H    Me  OMe  N                              II-241                                                                            Me     OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O H    OMe OMe  CH                             II-242                                                                            Me     OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O H    Me  OMe  CH                             II-243                                                                            Me     OCH.sub.2 CF.sub.2 CHF.sub.2                                                             H        O H    Me  OMe  N                              II-244                                                                            Me     OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O H    OMe OMe  CH                             II-245                                                                            Me     OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O H    Me  OMe  CH                             II-246                                                                            Me     OCH.sub.2 CF.sub.2 CF.sub.3                                                              H        O H    Me  OMe  N                              II-247                                                                            Me     OCH.sub.2 CHCl.sub.2                                                                     H        O H    OMe OMe  CH                             II-248                                                                            Me     OCH.sub.2 CHCl.sub.2                                                                     H        O H    Me  OMe  CH                             II-249                                                                            Me     OCH.sub.2 CHCl.sub.2                                                                     H        O H    Me  OMe  N                              II-250                                                                            Me     OCF.sub.2 CH.sub.2 Cl                                                                    H        O H    OMe OMe  CH                             II-251                                                                            Me     OCF.sub.2 CH.sub.2 Cl                                                                    H        O H    Me  OMe  CH                             II-252                                                                            Me     OCF.sub.2 CH.sub.2 Cl                                                                    H        O H    Me  OMe  N                              II-253                                                                            Me     OCF.sub.2 CHFCl                                                                          H        O H    OMe OMe  CH                             II-254                                                                            Me     OCF.sub.2 CHFCl                                                                          H        O H    Me  OMe  CH                             II-255                                                                            Me     OCF.sub.2 CHFCl                                                                          H        O H    Me  OMe  N                              II-256                                                                            Me     OCF.sub.3  H        O H    OMe OMe  CH                             II-257                                                                            Me     OCF.sub.3  H        O H    Me  OMe  CH                             II-258                                                                            Me     OCF.sub.3  H        O H    Me  OMe  N                              II-259                                                                            Me     OCH.sub.2 CHCHCl                                                                         H        O H    OMe OMe  CH                                                                              160-162                      II-260                                                                            Me     OCH.sub.2 CHCHCl                                                                         H        O H    Me  OMe  CH                             II-261                                                                            Me     OCH.sub.2 CHCHCl                                                                         H        O H    Me  OMe  N                              II-262                                                                            Me     OCH.sub.2 CHCCl.sub.2                                                                    H        O H    OMe OMe  CH                             II-263                                                                            Me     OCH.sub.2 CHCCl.sub.2                                                                    H        O H    Me  OMe  CH                             II-264                                                                            Me     OCH.sub.2 CHCCl.sub.2                                                                    H        O H    Me  OMe  N                              II-265                                                                            Me     OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O H    OMe OMe  CH                                                                              160-162                      II-266                                                                            Me     OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O H    Me  OMe  CH                             II-267                                                                            Me     OCH.sub.2 C(Cl)CH.sub.2                                                                  H        O H    Me  OMe  N                              II-268                                                                            Me     OCH.sub.2 C(Me)CH.sub.2                                                                  H        O H    OMe OMe  CH                                                                              163-164                      II-269                                                                            Me     OCH.sub.2 C(Me)CH.sub.2                                                                  H        O H    Me  OMe  CH                             II-270                                                                            Me     OCH.sub.2 C(Me)CH.sub.2                                                                  H        O H    Me  OMe  N                              II-271                                                                            Me     OCH.sub.2 CHCHMe                                                                         H        O H    OMe OMe  CH                             II-272                                                                            Me     OCH.sub.2 CHCHMe                                                                         H        O H    Me  OMe  CH                             II-273                                                                            Me     OCH.sub.2 CHCHMe                                                                         H        O H    Me  OMe  N                              II-274                                                                            Me     OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O H    OMe OMe  CH                             II-275                                                                            Me     OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O H    Me  OMe  CH                             II-276                                                                            Me     OCH.sub.2 CH.sub.2 N.sub.3                                                               H        O H    Me  OMe  N                              II-277                                                                            Me     OCH.sub.2 OMe                                                                            H        O H    OMe OMe  CH                                                                              165-167                      II-278                                                                            Me     OCH.sub.2 OMe                                                                            H        O H    Me  OMe  CH                             II-279                                                                            Me     OCH.sub.2 OMe                                                                            H        O H    Me  OMe  N                              II-280                                                                            Me     OCH.sub.2 OEt                                                                            H        O H    OMe OMe  CH                                                                              154-155                      II-281                                                                            Me     OCH.sub.2 OEt                                                                            H        O H    Me  OMe  CH                             II-282                                                                            Me     OCH.sub.2 OEt                                                                            H        O H    Me  OMe  N                              II-283                                                                            Me     OCH.sub.2 OBn                                                                            H        O H    OMe OMe  CH                                                                              162-164                      II-284                                                                            Me     OCH.sub.2 OBn                                                                            H        O H    Me  OMe  CH                             II-285                                                                            Me     OCH.sub.2 OBn                                                                            H        O H    Me  OMe  N                              II-286                                                                            Me     OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O H    OMe OMe  CH                             II-287                                                                            Me     OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O H    Me  OMe  CH                             II-288                                                                            Me     OCH.sub.2 OCH.sub.2 CF.sub.3                                                             H        O H    Me  OMe  N                              II-289                                                                            Me     OCH.sub.2 OBu-t                                                                          H        O H    OMe OMe  CH                             II-290                                                                            Me     OCH.sub.2 OBu-t                                                                          H        O H    Me  OMe  CH                             II-291                                                                            Me     OCH.sub.2 OBu-t                                                                          H        O H    Me  OMe  N                              II-292                                                                            Me     OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O H    OMe OMe  CH                             II-293                                                                            Me     OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O H    Me  OMe  CH                             II-294                                                                            Me     OCH.sub.2 OCH.sub.2 CH.sub.2 OMe                                                         H        O H    Me  OMe  N                              II-295                                                                            Me     OCH.sub.2 CN                                                                             H        O H    OMe OMe  CH                             II-296                                                                            Me     OCH.sub.2 CN                                                                             H        O H    Me  OMe  CH                             II-297                                                                            Me     OCH.sub.2 CN                                                                             H        O H    Me  OMe  N                              II-298                                                                            Me     OCH.sub.2 COOMe                                                                          H        O H    OMe OMe  CH                             II-299                                                                            Me     OCH.sub.2 COOMe                                                                          H        O H    Me  OMe  CH                             II-300                                                                            Me     OCH.sub.2 COOMe                                                                          H        O H    Me  OMe  N                              II-301                                                                            Me     OCH.sub.2 COOPr                                                                          H        O H    OMe OMe  CH                             II-302                                                                            Me     OCH.sub.2 COOPr                                                                          H        O H    Me  OMe  CH                             II-303                                                                            Me     OCH.sub.2 COOPr                                                                          H        O H    Me  OMe  N                              II-304                                                                            Me     OCH.sub.2 COOPr-i                                                                        H        O H    OMe OMe  CH                             II-305                                                                            Me     OCH.sub.2 COOPr-i                                                                        H        O H    Me  OMe  CH                             II-306                                                                            Me     OCH.sub.2 COOPr-i                                                                        H        O H    Me  OMe  N                              II-307                                                                            Me     OCH.sub.2 SMe                                                                            H        O H    OMe OMe  CH                             II-308                                                                            Me     OCH.sub.2 SMe                                                                            H        O H    Me  OMe  CH                             II-309                                                                            Me     OCH.sub.2 SMe                                                                            H        O H    Me  OMe  N                              II-310                                                                            Me     OCH.sub.2 CH.sub.2 SMe                                                                   H        O H    OMe OMe  CH                             II-311                                                                            Me     OCH.sub.2 CH.sub.2 SMe                                                                   H        O H    Me  OMe  CH                             II-312                                                                            Me     OCH.sub.2 CH.sub.2 SMe                                                                   H        O H    Me  OMe  N                              II-313                                                                            Me     SCF.sub.3  H        O H    OMe OMe  CH                             II-314                                                                            Me     SCF.sub.3  H        O H    Me  OMe  CH                             II-315                                                                            Me     SCF.sub.3  H        O H    Me  OMe  N                              II-316                                                                            Me     SCH.sub.2 CH.sub.2 Cl                                                                    H        O H    OMe OMe  CH                             II-317                                                                            Me     SCH.sub.2 CH.sub.2 Cl                                                                    H        O H    Me  OMe  CH                             II-318                                                                            Me     SCH.sub.2 CH.sub.2 Cl                                                                    H        O H    Me  OMe  N                              II-319                                                                            Me     SCH.sub.2 CH.sub.2 F                                                                     H        O H    OMe OMe  CH                             II-320                                                                            Me     SCH.sub.2 CH.sub.2 F                                                                     H        O H    Me  OMe  CH                             II-321                                                                            Me     SCH.sub.2 CH.sub.2 F                                                                     H        O H    Me  OMe  N                              II-322                                                                            Me     SOEt       H        O H    OMe OMe  CH                             II-323                                                                            Me     SOEt       H        O H    Me  OMe  CH                             II-324                                                                            Me     SOEt       H        O H    Me  OMe  N                              II-325                                                                            Me     SO.sub.2 NHOEt                                                                           H        O H    OMe OMe  CH                             II-326                                                                            Me     SO.sub.2 NHOEt                                                                           H        O H    Me  OMe  CH                             II-327                                                                            Me     SO.sub.2 NHOEt                                                                           H        O H    Me  OMe  N                              II-328                                                                            Me     SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O H    OMe OMe  CH                             II-329                                                                            Me     SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O H    Me  OMe  CH                             II-330                                                                            Me     SO.sub.2 CH.sub.2 CHCH.sub.2                                                             H        O H    Me  OMe  N                              II-331                                                                            Me     SO.sub.2 NEt.sub.2                                                                       H        O H    OMe OMe  CH                             II-332                                                                            Me     SO.sub.2 NEt.sub.2                                                                       H        O H    Me  OMe  CH                             II-333                                                                            Me     SO.sub.2 NEt.sub.2                                                                       H        O H    Me  OMe  N                              II-334                                                                            Me     Et         H        O H    OMe OMe  CH                             II-335                                                                            Me     Et         H        O H    Me  OMe  CH                             II-336                                                                            Me     Et         H        O H    Me  OMe  N                              II-337                                                                            Me     Pr         H        O H    OMe OMe  CH                             II-338                                                                            Me     Pr         H        O H    Me  OMe  CH                             II-339                                                                            Me     Pr         H        O H    OMe OMe  N                              II-340                                                                            Me     Pr-i       H        O H    OMe OMe  CH                             II-341                                                                            Me     Pr-i       H        O H    Me  OMe  CH                             II-342                                                                            Me     Pr-i       H        O H    Me  OMe  N                              II-343                                                                            Me     Bu         H        O H    OMe OMe  CH                             II-344                                                                            Me     Bu         H        O H    Me  OMe  CH                             II-345                                                                            Me     Bu         H        O H    Me  OMe  N                              II-346                                                                            Me     Bu-t       H        O H    OMe OMe  CH                             II-347                                                                            Me     Bu-t       H        O H    Me  OMe  CH                             II-348                                                                            Me     Bu-t       H        O H    Me  OMe  N                              II-349                                                                            Me     CH.sub.2 Cl                                                                              H        O H    OMe OMe  CH                             II-350                                                                            Me     CH.sub.2 Cl                                                                              H        O H    Me  OMe  CH                             II-351                                                                            Me     CH.sub.2 Cl                                                                              H        O H    Me  OMe  N                              II-352                                                                            Me     CH.sub.2 F H        O H    OMe OMe  CH                             II-353                                                                            Me     CH.sub.2 F H        O H    Me  OMe  CH                             II-354                                                                            Me     CH.sub.2 F H        O H    Me  OMe  N                              II-355                                                                            Me     CH.sub.2 OMe                                                                             H        O H    OMe OMe  CH                             II-356                                                                            Me     CH.sub.2 OMe                                                                             H        O H    Me  OMe  CH                             II-357                                                                            Me     CH.sub.2 OMe                                                                             H        O H    Me  OMe  N                              II-358                                                                            Me     CH.sub.2 CF.sub.3                                                                        H        O H    OMe OMe  CH                             II-359                                                                            Me     CH.sub.2 CF.sub.3                                                                        H        O H    Me  OMe  CH                             II-360                                                                            Me     CH.sub.2 CF.sub.3                                                                        H        O H    Me  OMe  N                              II-361                                                                            Me                                                                                    ##STR44## H        O H    OMe OMe  CH                             II-362                                                                            Me                                                                                    ##STR45## H        O H    Me  OMe  CH                             II-363                                                                            Me                                                                                    ##STR46## H        O H    Me  OMe  N                              II-364                                                                            Me     CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O H    OMe OMe  CH                             II-365                                                                            Me     CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O H    Me  OMe  CH                             II-366                                                                            Me     CH.sub.2 CH.sub.2 CF.sub.3                                                               H        O H    Me  OMe  N                              II-367                                                                            Me     CH.sub.2 CHCH.sub.2                                                                      H        O H    OMe OMe  CH                             II-368                                                                            Me     CH.sub.2 CHCH.sub.2                                                                      H        O H    Me  OMe  CH                             II-369                                                                            Me     CH.sub.2 CHCH.sub.2                                                                      H        O H    Me  OMe  N                              II-370                                                                            Me     CH.sub.2 C CH                                                                            H        O H    OMe OMe  CH                             II-371                                                                            Me     CH.sub.2 C CH                                                                            H        O H    Me  OMe  CH                             II-372                                                                            Me     CH.sub.2 C CH                                                                            H        O H    Me  OMe  N                              II-373                                                                            Me     CH.sub.2 COOMe                                                                           H        O H    OMe OMe  CH                             II-374                                                                            Me     CH.sub.2 COOMe                                                                           H        O H    Me  OMe  CH                             II-375                                                                            Me     CH.sub.2 COOMe                                                                           H        O H    Me  OMe  N                              II-376                                                                            Me     CH.sub.2 COOEt                                                                           H        O H    OMe OMe  CH                             II-377                                                                            Me     CH.sub.2 COOEt                                                                           H        O H    Me  OMe  CH                             II-378                                                                            Me     CH.sub.2 COOEt                                                                           H        O H    Me  OMe  N                              II-379                                                                            Me     CH.sub.2 CN                                                                              H        O H    OMe OMe  CH                             II-380                                                                            Me     CH.sub.2 CN                                                                              H        O H    Me  OMe  CH                             II-381                                                                            Me     CH.sub.2 CN                                                                              H        O H    Me  OMe  N                              II-382                                                                            Me     CH.sub.2 CONMe.sub.2                                                                     H        O H    OMe OMe  CH                             II-383                                                                            Me     CH.sub.2 CONMe.sub.2                                                                     H        O H    Me  OMe  CH                             II-384                                                                            Me     CH.sub.2 CONMe.sub.2                                                                     H        O H    Me  OMe  N                              II-385                                                                            Me     CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O H    OMe OMe  CH                             II-386                                                                            Me     CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O H    Me  OMe  CH                             II-387                                                                            Me     CH.sub.2 SO.sub.2 NMe.sub.2                                                              H        O H    Me  OMe  N                              II-388                                                                            Me     CH.sub.2 NMe.sub.2                                                                       H        O H    OMe OMe  CH                             II-389                                                                            Me     CH.sub.2 NMe.sub.2                                                                       H        O H    Me  OMe  CH                             II-390                                                                            Me     CH.sub.2 NMe.sub.2                                                                       H        O H    Me  OMe  N                              II-391                                                                            Me     CHCH.sub.2 H        O H    OMe OMe  CH                             II-392                                                                            Me     CHCH.sub.2 H        O H    Me  OMe  CH                             II-393                                                                            Me     CHCH.sub.2 H        O H    Me  OMe  N                              II-394                                                                            Me     CHCHMe     H        O H    OMe OMe  CH                             II-395                                                                            Me     CHCHMe     H        O H    Me  OMe  CH                             II-396                                                                            Me     CHCHMe     H        O H    Me  OMe  N                              II-397                                                                            Me     C CH       H        O H    OMe OMe  CH                             II-398                                                                            Me     C CH       H        O H    Me  OMe  CH                             II-399                                                                            Me     C CH       H        O H    Me  OMe  N                              II-400                                                                            Me     C CMe      H        O H    OMe OMe  CH                             II-401                                                                            Me     C CMe      H        O H    Me  OMe  CH                             II-402                                                                            Me     C CMe      H        O H    Me  OMe  N                              II-403                                                                            Me     CHCHCOOMe  H        O H    OMe OMe  CH                             II-404                                                                            Me     CHCHCOOMe  H        O H    Me  OMe  CH                             II-405                                                                            Me     CHCHCOOMe  H        O H    Me  OMe  N                              II-406                                                                            Me     CH(Me)COMe H        O H    OMe OMe  CH                             II-407                                                                            Me     CH(Me)COMe H        O H    Me  OMe  CH                             II-408                                                                            Me     CH(Me)COMe H        O H    Me  OMe  N                              II-409                                                                            Me     CH(Me)COEt H        O H    OMe OMe  CH                             II-410                                                                            Me     CH(Me)COEt H        O H    Me  OMe  CH                             II-411                                                                            Me     CH(Me)COEt H        O H    Me  OMe  N                              II-412                                                                            Me     CH(Et)COMe H        O H    OMe OMe  CH                             II-413                                                                            Me     CH(Et)COMe H        O H    Me  OMe  CH                             II-414                                                                            Me     CH(Et)COMe H        O H    Me  OMe  N                              II-415                                                                            Me     CH(Et)COEt H        O H    OMe OMe  CH                             II-416                                                                            Me     CH(Et)COEt H        O H    Me  OMe  CH                             II-417                                                                            Me     CH(Et)COEt H        O H    Me  OMe  N                              II-418                                                                            Me                                                                                    ##STR47## H        O H    OMe OMe  CH                             II-419                                                                            Me                                                                                    ##STR48## H        O H    Me  OMe  CH                             II-420                                                                            Me                                                                                    ##STR49## H        O H    Me  OMe  N                              II-421                                                                            Me     COPr       H        O H    OMe OMe  CH                             II-422                                                                            Me     COPr       H        O H    Me  OMe  CH                             II-423                                                                            Me     COPr       H        O H    Me  OMe  N                              II-424                                                                            Me     COPr-i     H        O H    OMe OMe  CH                             II-425                                                                            Me     COPr-i     H        O H    Me  OMe  CH                             II-426                                                                            Me     COPr-i     H        O H    Me  OMe  N                              II-427                                                                            Me     CHNOMe     H        O H    OMe OMe  CH                             II-428                                                                            Me     CHNOMe     H        O H    Me  OMe  CH                             II-429                                                                            Me     CHNOMe     H        O H    Me  OMe  N                              II-430                                                                            Me     CHNOEt     H        O H    OMe OMe  CH                             II-431                                                                            Me     CHNOEt     11       O H    Me  OMe  CH                             II-432                                                                            Me     CHNOEt     H        O H    Me  OMe  N                              II-433                                                                            Me     C(Me)NOMe  H        O H    OMe OMe  CH                             II-434                                                                            Me     C(Me)NOMe  H        O H    Me  OMe  CH                             II-435                                                                            Me     C(Me)NOMe  H        O H    Me  OMe  N                              II-436                                                                            Me     C(Me)NOEt  H        O H    OMe OMe  CH                             II-437                                                                            Me     C(Me)NOEt  H        O H    Me  OMe  CH                             II-438                                                                            Me     C(Me)NOEt  H        O H    Me  OMe  N                              II-439                                                                            Me     C(Me)NOPr  H        O H    OMe OMe  CH                             II-440                                                                            Me     C(Me)NOPr  H        O H    Me  OMe  CH                             II-441                                                                            Me     C(Me)NOPr  H        O H    Me  OMe  N                              II-442                                                                            Me     C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O H    OMe OMe  CH                             II-443                                                                            Me     C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O H    Me  OMe  CH                             II-444                                                                            Me     C(Me)NOCH.sub.2 CH.sub.2 Cl                                                              H        O H    Me  OMe  N                              II-445                                                                            Me     C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O H    OMe OMe  CH                             II-446                                                                            Me     C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O H    Me  OMe  CH                             II-447                                                                            Me     C(Me)NOCH.sub.2 CH.sub.2 F                                                               H        O H    Me  OMe  N                              II-448                                                                            Me     NHEt       H        O H    OMe OMe  CH                             II-449                                                                            Me     NHEt       H        O H    Me  OMe  CH                             II-450                                                                            Me     NHEt       H        O H    Me  OMe  N                              II-451                                                                            Me     NHPr       H        O H    OMe OMe  CH                             II-452                                                                            Me     NHPr       H        O H    Me  OMe  CH                             II-453                                                                            Me     NHPr       H        O H    Me  OMe  N                              II-454                                                                            Me     NHCOOMe    H        O H    OMe OMe  CH                             II-455                                                                            Me     NHCOOMe    H        O H    Me  OMe  CH                             II-456                                                                            Me     NHCOOMe    H        O H    Me  OMe  N                              II-457                                                                            Me     NHCOOEt    H        O H    OMe OMe  CH                             II-458                                                                            Me     NHCOOEt    H        O H    Me  OMe  CH                             II-459                                                                            Me     NHCOOEt    H        O H    Me  OMe  N                              II-460                                                                            Me     NHCOOPh    H        O H    OMe OMe  CH                             II-461                                                                            Me     NHCOOPh    H        O H    Me  OMe  CH                             II-462                                                                            Me     NHCOOPh    H        O H    Me  OMe  N                              II-463                                                                            Me     N(Me)SO.sub.2 Me                                                                         H        O H    OMe OMe  CH                             II-464                                                                            Me     N(Me)SO.sub.2 Me                                                                         H        O H    Me  OMe  CH                             II-465                                                                            Me     N(Me)SO.sub.2 Me                                                                         H        O H    Me  OMe  N                              II-466                                                                            Me     N(Et)SO.sub.2 Me                                                                         H        O H    OMe OMe  CH                             II-467                                                                            Me     N(Et)SO.sub.2 Me                                                                         H        O H    Me  OMe  CH                             II-468                                                                            Me     N(Et)SO.sub.2 Me                                                                         H        O H    Me  OMe  N                              II-469                                                                            Me     N(Me)SO.sub.2 Et                                                                         H        O H    OMe OMe  CH                             II-470                                                                            Me     N(Me)SO.sub.2 Et                                                                         H        O H    Me  OMe  CH                             II-471                                                                            Me     N(Me)SO.sub.2 Et                                                                         H        O H    Me  OMe  N                              II-472                                                                            Me     N(Et)SO.sub.2 Et                                                                         H        O H    OMe OMe  CH                             II-473                                                                            Me     N(Et)SO.sub.2 Et                                                                         H        O H    Me  OMe  CH                             II-474                                                                            Me     N(Et)SO.sub.2 Et                                                                         H        O H    Me  OMe  N                              II-475                                                                            Me     NHCOEt     H        O H    OMe OMe  CH                             II-476                                                                            Me     NHCOEt     H        O H    Me  OMe  CH                             II-477                                                                            Me     NHCOEt     H        O H    Me  OMe  N                              II-478                                                                            Me     NHCOCF.sub.3                                                                             H        O H    OMe OMe  CH                             II-479                                                                            Me     NHCOCF.sub.3                                                                             H        O H    Me  OMe  CH                             II-480                                                                            Me     NHCOCF.sub.3                                                                             H        O H    Me  OMe  N                              II-481                                                                            Me     NCHMe      H        O H    OMe OMe  CH                             II-482                                                                            Me     NCHMe      H        O H    Me  OMe  CH                             II-483                                                                            Me     NCHMe      H        O H    Me  OMe  N                              II-484                                                                            Me     NCHPh      H        O H    OMe OMe  CH                             II-485                                                                            Me     NCHPh      H        O H    Me  OMe  CH                             II-486                                                                            Me     NCHPh      H        O H    Me  OMe  N                              II-487                                                                            Me     N.sub.3    H        O H    OMe OMe  CH                             II-488                                                                            Me     N.sub.3    H        O H    Me  OMe  CH                             II-489                                                                            Me     N.sub.3    H        O H    Me  OMe  N                              II-490                                                                            Me     I          H        O H    OMe OMe  CH                             II-491                                                                            Me     I          H        O H    Me  OMe  CH                             II-492                                                                            Me     I          H        O H    Me  OMe  N                              II-493                                                                            Me     OCOEt      H        O H    OMe OMe  CH                             II-494                                                                            Me     OCOEt      H        O H    Me  OMe  CH                             II-495                                                                            Me     OCOEt      H        O H    Me  OMe  N                              II-496                                                                            Me     OCOPr      H        O H    OMe OMe  CH                             II-497                                                                            Me     OCOPr      H        O H    Me  OMe  CH                             II-498                                                                            Me     OCOPt      H        O H    Me  OMe  N                              II-499                                                                            Me     OCOPh      H        O H    OMe OMe  CH                             II-500                                                                            Me     OCOPh      H        O H    Me  OMe  CH                             II-501                                                                            Me     OCOPh      H        O H    Me  OMe  N                              II-502                                                                            Me     OCONMe.sub.2                                                                             H        O H    OMe OMe  CH                             II-503                                                                            Me     OCONMe.sub.2                                                                             H        O H    Me  OMe  CH                             II-504                                                                            Me     OCONMe.sub.2                                                                             H        O H    Me  OMe  N                              II-505                                                                            Me     Cl         H        O H    CF.sub.3                                                                          OMe  CH                             II-506                                                                            Me     OPr-i      H        O H    Cl  OMe  CH                             II-507                                                                            Me     SEt        H        O H    Me  OMe  CH                             II-508                                                                            Me     SEt        H        O H    Cl  OMe  CH                             II-509                                                                            Me     SEt        H        O H    Me  Me   CH                             II-510                                                                            Me     SEt        H        O H    OMe OMe  N                              II-511                                                                            Me     SBu        H        O H    OMe Me   CH                             II-512                                                                            Me     SBu        H        O H    OMe Me   N                              II-513                                                                            Me     SPr-i      H        O H    OMe Me   CH                             II-514                                                                            Me     SPr-i      H        O H    OMe Me   N                              II-515                                                                            Me     SOEt       H        O H    OMe OMe  N                              II-516                                                                            Me     SO.sub.2 Et                                                                              H        O H    OMe Me   CH                             II-517                                                                            Me     SO.sub.2 Et                                                                              H        O H    OMe Me   N                              II-518                                                                            Me     SO.sub.2 Et                                                                              H        O H    OMe Cl   CH                             II-519                                                                            Me     SO.sub.2 Pr                                                                              H        O H    OMe Me   CH                             II-520                                                                            Me     SO.sub.2 Pr                                                                              H        O H    OMe Me   N                              II-521                                                                            Me     SO.sub.2 Pr                                                                              H        O H    OMe Cl   CH                             II-522                                                                            Me     SO.sub.2 Bu                                                                              H        O H    OMe Me   CH                             II-523                                                                            Me     SO.sub.2 Bu                                                                              H        O H    OMe Me   N                              II-524                                                                            Me     SO.sub.2 Bu                                                                              H        O H    OMe Cl   CH                             II-525                                                                            Me     SO.sub.2 Pr-i                                                                            H        O H    OMe Me   CH                             II-526                                                                            Me     SO.sub.2 Pr-i                                                                            H        O H    OMe Me   N                              II-527                                                                            Me     COOPr      H        O H    OMe Me   N                              II-528                                                                            Me     NO.sub.2   H        O H    OMe Cl   CH                             II-529                                                                            Me     CONMe.sub.2                                                                              H        O H    OMe Me   CH                             II-530                                                                            Me     Br         H        O H    OMe Cl   CH                             II-531                                                                            Me                                                                                    ##STR50## H        O H    OMe OMe  CH                                                                              156-158                      II-532                                                                            Me     OCH.sub.2 Bu-t                                                                           H        O H    OMe OMe  CH                                                                              144-146                      II-533                                                                            Me     OCH.sub.2 Bu-t                                                                           H        O H    Me  OMe  CH                                                                              126-128                      II-534                                                                            Me     OCH.sub.2 CHCMe.sub.2                                                                    H        O H    OMe OMe  CH                                                                              164-166                      II-535                                                                            Me     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O H    OMe OMe  CH                                                                              136-138                      II-536                                                                            Me     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O H    Me  OMe  CH                                                                              173-175                      II-537                                                                            Me     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                            H        O H    Me  OMe  N 160-163                      II-538                                                                            Me     CH.sub.2 CH.sub.2 N.sub.3                                                                H        O H    OMe OMe  CH                             II-539                                                                            Me                                                                                    ##STR51## H        O H    OMe OMe  CH                             II-540                                                                            Me     COCF.sub.3 H        O H    OMe OMe  CH                             II-541                                                                            Me     COOCH.sub.2 CHCHCl                                                                       H        O H    OMe OMe  CH                             II-542                                                                            Me     SO.sub.2 CF.sub.3                                                                        H        O H    OMe OMe  CH                             II-543                                                                            Me     OCOCF.sub.3                                                                              H        O H    OMe OMe  CH                             II-544                                                                            Me     OCH.sub.2 OPh                                                                            H        O H    OMe OMe  CH                             II-545                                                                            Me     CHNOH      H        O H    OMe OMe  CH                             II-546                                                                            Me     CHNOCH.sub.2 CHCH.sub.2                                                                  H        O H    OMe OMe  CH                             II-547                                                                            Me     CHNOCH.sub.2 C CH                                                                        H        O H    OMe OMe  CH                             II-548                                                                            Me     C(Me)NOBn  H        O H    OMe OMe  CH                             II-549                                                                            Me     C(Me)NOPh  H        O H    OMe OMe  CH                             II-550                                                                            Me     C(Bn)NOMe  H        O H    OMe OMe  CH                             II-551                                                                            Me     C(Ph)NOMe  H        O H    OMe OMe  CH                             II-552                                                                            Me     C(CF.sub.3)NOMe                                                                          H        O H    OMe OMe  CH                             II-553                                                                            Me     COOCH.sub.2 CH.sub.2 Cl                                                                  H        O H    OMe OMe  CH                             II-554                                                                            Me     COOCH.sub.2 CF.sub.3                                                                     H        O H    OMe OMe  CH                             II-555                                                                            Me     Cl         5-Cl     O H    OMe Me   N                              II-556                                                                            Me     Cl         5-OMe    O H    OMe OMe  CH                                                                              197-199                      II-557                                                                            Me     Cl         5-F      O H    OMe OMe  CH                             II-558                                                                            Me     F          5-Cl     O H    OMe OMe  CH                             II-559                                                                            Me     F          5-F      O H    OMe OMe  CH                             II-560                                                                            Me     COOMe      5-Cl     O H    OMe OMe  CH                             II-561                                                                            Me     COOEt      5-Cl     O H    OMe OMe  CH                             II-562                                                                            Me     COOPr      5-Cl     O H    OMe OMe  CH                             II-563                                                                            Me     COOPr-i    5-Cl     O H    OMe OMe  CH                             II-564                                                                            Me     OMe        5-COOMe  O H    OMe OMe  CH                             II-565                                                                            Me     COOMe      5-OMe    O H    OMe OMe  CH                             II-566                                                                            Me     H          5-CN     O H    OMe OMe  CH                             II-567                                                                            Me     H          5-CF.sub.3                                                                             O H    OMe OMe  CH                             II-568                                                                            Me     H          5-COOMe  O H    OMe OMe  CH                             II-569                                                                            Me     H          5-COOEt  O H    OMe OMe  CH                             II-570                                                                            Me     H          5-COOPr  O H    OMe OMe  CH                             II-571                                                                            Me     H          5-COOPr-i                                                                              O H    OMe OMe  CH                             II-572                                                                            Me     H          5-COOCH.sub.2 CH.sub.2 Cl                                                              O H    OMe OMe  CH                             II-573                                                                            Me     H          5-COOCH.sub.2 CH.sub.2 F                                                               O H    OMe OMe  CH                             II-574                                                                            Me     H          5-COOCH.sub.2 CF.sub.3                                                                 O H    OMe OMe  CH                             II-575                                                                            Me     H          5-COOCH.sub.2 OMe                                                                      O H    OMe OMe  CH                             II-576                                                                            Me     H          5-CONMe.sub.2                                                                          O H    OMe OMe  CH                             II-577                                                                            Me     H          5-OCH.sub.2 CH.sub.2 F                                                                 O H    OMe OMe  CH                             II-578                                                                            Me     H          5-OCHF.sub.2                                                                           O H    OMe OMe  CH                             II-579                                                                            Me     H          5-OCH.sub.2 CF.sub.3                                                                   O H    OMe OMe  CH                             II-580                                                                            Me     H          5-OCH.sub.2 CH.sub.2 CH.sub.2 F                                                        O H    OMe OMe  CH                             II-581                                                                            Me     H          5-OCH.sub.2 CHCH.sub.2                                                                 O H    OMe OMe  CH                             II-582                                                                            Me     H          5-OCH.sub.2 C CH                                                                       O H    OMe OMe  CH                             II-583                                                                            Me     H          5-NO.sub.2                                                                             O H    OMe OMe  CH                             II-584                                                                            Me     H          5-SMe    O H    OMe OMe  CH                             II-585                                                                            Me     H          5-SEt    O H    OMe OMe  CH                             II-586                                                                            Me     H          5-SPr    O H    OMe OMe  CH                             II-587                                                                            Me     H          5-SPr-i  O H    OMe OMe  CH                             II-588                                                                            Me     H          5-SO.sub.2 Et                                                                          O H    OMe OMe  CH                             II-589                                                                            Me     H          5-SO.sub.2 Pr                                                                          O H    OMe OMe  CH                             II-590                                                                            Me     H          5-SO.sub.2 Pr-i                                                                        O H    OMe OMe  CH                             II-591                                                                            Me     H          5-SOEt   O H    OMe OMe  CH                             II-592                                                                            Me     H          5-Me     O H    OMe OMe  CH                             II-593                                                                            Me     H          S-Et     O H    OMe OMe  CH                             II-594                                                                            Me     H          5-Pr     O H    OMe OMe  CH                             II-595                                                                            Me     H          5-SO.sub.2 NMe.sub.2                                                                   O H    OMe OMe  CH                             II-596                                                                            Me     H          5-OCF.sub.3                                                                            O H    OMe OMe  CH                             II-597                                                                            Me     H          5-CH.sub.2 CF.sub.3                                                                    O H    OMe OMe  CH                             II-598                                                                            Me     H          5-CH.sub.2 CHCH.sub.2                                                                  O H    OMe OMe  CH                             II-599                                                                            Me     H          5-COOMe  O H    OMe Me   CH                             II-600                                                                            Me     H          5-COOMe  O H    OMe Me   N                              II-601                                                                            Me     H          5-COOMe  O H    OMe OMe  N                              II-602                                                                            Me                                                                                    ##STR52## H        O H    OMe OMe  CH                             II-603                                                                            Me                                                                                    ##STR53## H        O H    Me  OMe  CH                             II-604                                                                            Me                                                                                    ##STR54## H        O H    Me  OMe  N                              II-605                                                                            Me                                                                                    ##STR55## H        O H    OMe OMe  CH                             II-606                                                                            Me                                                                                    ##STR56## H        O H    Me  OMe  CH                             II-607                                                                            Me                                                                                    ##STR57## H        O H    Me  OMe  N                              II-608                                                                            Me                                                                                    ##STR58## H        O H    OMe OMe  CH                             II-609                                                                            Me                                                                                    ##STR59## H        O H    Me  OMe  CH                             II-610                                                                            Me                                                                                    ##STR60## H        O H    Me  OMe  N                              II-611                                                                            Me     OC.sub.2 H.sub.4 O*                                                                      O        H OMe  OMe CH                                  II-612                                                                            Me     OC.sub.2 H.sub.4 O*                                                                      O        H Me   OMe CH                                  II-613                                                                            Me     OC.sub.2 H.sub.4 O*                                                                      O        H Me   OMe N                                   II-614                                                                            Me     SC.sub.2 H.sub.4 S*                                                                      O        H OMe  OMe CH                                  II-615                                                                            Me     SC.sub.2 H.sub.4 S*                                                                      O        H Me   OMe CH                                  II-616                                                                            Me     SC.sub.2 H.sub.4 S*                                                                      O        H Me   OMe N                                   II-617                                                                            Me     OCH.sub.2 O*                                                                             O        H OMe  OMe CH                                  II-618                                                                             ##STR61##                                                                           Cl         H        O H    OMe OMe  CH                             II-619                                                                             ##STR62##                                                                           Cl         H        O H    OMe OMe  CH                             II-620                                                                             ##STR63##                                                                           Cl         H        O H    OMe OMe  CH                             II-621                                                                            COMe   Cl         H        O H    OMe OMe  CH                             II-622                                                                            COEt   Cl         H        O H    OMe OMe  CH                             II-623                                                                            COPr   Cl         H        O H    OMe OMe  CH                             II-624                                                                            COPr-i Cl         H        O H    OMe OMe  CH                             II-625                                                                            COPh   Cl         H        O H    OMe OMe  CH                             II-626                                                                            SO.sub.2 Me                                                                          Cl         H        O H    OMe OMe  CH                             II-627                                                                            SO.sub.2 Et                                                                          Cl         H        O H    OMe OMe  CH                             II-628                                                                            SO.sub.2 Ph                                                                          Cl         H        O H    OMe OMe  CH                             II-629                                                                            COOMe  Cl         H        O H    OMe OMe  CH                             II-630                                                                            COOEt  Cl         H        O H    OMe OMe  CH                             II-631                                                                            COOPh  Cl         H        O H    OMe OMe  CH                             II-632                                                                            CONMe.sub.2                                                                          Cl         H        O H    OMe OMe  CH                             II-633                                                                            SO.sub.2 NMe.sub.2                                                                   Cl         H        O H    OMe OMe  CH                             II-634                                                                            Ph     Cl         H        O H    Me  OMe  N                              II-635                                                                            CH.sub.2 OMe                                                                         Cl         H        O H    OMe OMe  CH                             II-636                                                                            CH.sub.2 OBn                                                                         Cl         H        O H    OMe OMe  CH                             II-637                                                                            CH.sub.2 CH.sub.2 F                                                                  Cl         H        O H    OMe OMe  CH                             II-638                                                                            CH.sub.2 CH.sub.2 Cl                                                                 Cl         H        O H    OMe OMe  CH                             II-639                                                                            CF.sub.3                                                                             Cl         H        O H    OMe OMe  CH                             II-640                                                                            CH.sub.2 F                                                                           Cl         H        O H    OMe OMe  CH                             II-641                                                                            CH.sub.2 CHCH.sub.2                                                                  OMe        H        O H    OMe OMe  CH                             II-642                                                                            COCF.sub.3                                                                           Cl         H        O H    OMe OMe  CH                             II-643                                                                             ##STR64##                                                                           Cl         H        O H    OMe OMe  CH                             II-644                                                                            Me     Cl         H        O CH.sub.3 OCH.sub.2                                                                 OMe OMe  CH                             II-645                                                                            Me     Cl         H        O H    OMe NMe.sub.2                                                                          N                              II-646                                                                            Me     Cl         H        O H    OMe NHMe N                              II-648                                                                            Me     ONCHMe     H        O H    OMe OMe  CH                             II-649                                                                            Me     ONCMe.sub.2                                                                              H        O H    OMe OMe  CH                             II-650                                                                            Me     ONCHBn     H        O H    OMe OMe  CH                             II-651                                                                            Me     OCH.sub.2 CH.sub.2 F                                                                     H        O H    OMe Me   CH                                                                              167-170                      II-652                                                                            Me     OCH.sub.2 CH.sub.2 F                                                                     H        O H    OMe Me   N 167-169                      II-653                                                                            Me     F          H        O H    NMe.sub.2                                                                         OCH.sub.2 CF.sub.3                                                                 N 108-112                      II-654                                                                            Me     SO.sub.2 NMe.sub.2                                                                       H        O H    OMe Me   N 191-193                      II-655                                                                            Me     CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            H        O H    OMe OMe  CH                             II-656                                                                            Me     CO.sub.2 CH.sub.2 CF.sub.3                                                               H        O H    OMe OMe  CH                             II-657                                                                            Me     CO.sub.2 CH.sub.2 OMe                                                                    H        O H    OMe OMe  CH                             II-658                                                                            H      CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            H        O H    OMe OMe  CH                             II-659                                                                            H      CO.sub.2 CH.sub.2 CF.sub.3                                                               H        O H    OMe OMe  CH                             II-660                                                                            H      CO.sub.2 CH.sub.2 OMe                                                                    H        O H    OMe OMe  CH                             __________________________________________________________________________     *R.sup.3 represents the 5 position.                                      

The following processes may, for example, be mentioned as the processesfor producing the compounds of the present invention. However, theprocesses are not limited to such specific processes.

Common processes for producing the compound I! or II! of the presentinvention are shown by the following Processes 1 to 3. ##STR65##(wherein R¹, R², R³, A, B, Z, X and Y have the same meanings as definedabove.)

Namely, the compound of the present invention represented by the formulaI! or II! can be produced by reacting an intermediate for its productionof the present invention represented by the formula I-a! or II-a!(hereinafter referred to as an intermediate, and the process for itsproduction will be described hereinafter) and a compound represented bythe formula III!.

This reaction is usually conducted in a solvent or without solvent, ifnecessary, in the presence of a base. The range of the reactiontemperature is a range from -20° C. to the boiling point of the solvent,and the range of the reaction time is a range of from 0.5 hour to 24hours. With respect to the amounts of the compounds to be subjected tothe reaction, the amounts of the compound represented by the formulaIII! and the base are respectively independently from 1 to 1.5equivalent relative to one equivalent of the intermediate represented bythe formula I-a! or II-a!.

As the solvent, an aromatic hydrocarbon such as benzene, xylene ortoluene, a halogenated hydrocarbon such as chloroform, carbontetrachloride, dichloroethane, chlorobenzene or dichlorobenzene, anether such as diethyl ether, dioxane, tetrahydrofuran (THF), isopropylether (IPE) or diethylene glycol dimethyl ether, an alcohol such asmethanol, ethanol or 2-propanol, an ester such as ethyl acetate or butylacetate, a nitro compound such as nitromethane or nitrobenzene, anitrile such as acetonitrile or isobutyronitrile, or an aprotic polarsolvent such as formamide, N,N-dimethylformamide (DMF),N,N-dimethylacetamide (DMAC), dimethylsulfoxide (DMSO) orN-methylpyrrolidone (NMP), may, for example, be mentioned.

As the base, an organic base such as pyridine, triethylamine,1,4-diazabicyclo 2.2.2!octane, 1,8-diazabicyclo 5.4.0!-7-undecene (DBU),N,N-diethylaniline or diethyl-methylamine, an inorganic base such assodium hydroxide, potassium hydroxide, sodium carbonate, potassiumcarbonate or sodium hydride, or an alkali metal alkoxide such as sodiummethoxide or sodium ethoxide, may, for example, be mentioned.

Further, the compound represented by the formula III! can be produced byreacting a compound represented by the formula IV! in Process 2 withphenyl chloroformate, phenyl chlorothio-O-formate or phenylchlorodithioformate, in a proper solvent in the presence of a base.##STR66## (wherein R¹, R², R³, A, B, X, Y and Z have the same meaningsas defined above.)

The compound of the present invention represented by the formula I! orII! can be produced by reacting a compound represented by the formulaI-b! or II-b! and a compound represented by the formula IV!. Thecompound represented by the formula I-b! or II-b! can be produced byreacting an intermediate represented by the formula I-a! or II-a! withphosgene or thiophosgene in a suitable solvent.

This reaction is usually conducted in a solvent or without solvent, ifnecessary, in the presence of a base. The range of the reactiontemperature, the range of the reaction time, and the solvent and thebase to be used in the reaction are the same as in Process 1. Withrespect to the amounts of the compounds to be subjected to the reaction,the amounts of the compounds represented by the formula IV! and the baseare respectively independently from 1 to 1.5 equivalent relative to oneequivalent of the compound represented by the formula I-b! or II-b!.##STR67## (wherein R¹, R², R³, A, B, X, Y and Z have the same meaningsas defined above.)

The compound of the present invention represented by the formula I! orII! can be produced by reacting a compound represented by the formulaI-c! or II-c! and a compound of the formula IV!. The compoundrepresented by the formula I-c! or II-c! can be produced by reacting anintermediate represented by the formula I-a! or II-a! with phenylchloroformate, phenyl chlorothio-O-formate or phenylchlorodithioformate, in a suitable solvent in the presence of a base. Itmay also be produced by reacting a compound represented by the formulaI-b! or II-b! with phenol or thiophenol.

This reaction is usually conducted in a solvent or without solvent, ifnecessary, in the presence of a base. The range of the reactiontemperature, the range of the reaction time, and the solvent and thebase to be used in the reaction are the same as in Process 1. Withrespect to the amounts of the compounds to be subjected to the reaction,the amounts of the compound represented by the formula IV! and the baseare respectively independently from 1 to 1.5 equivalent relative to oneequivalent of the compound represented by the formula I-c! or II-c!. Aprocess for producing an intermediate of the formula I-a! useful for theproduction of the compound of the present invention will be shown byProcess 1 For Producing An Intermediate, and a process for producing anintermediate of the formula II-a! will be shown by Process 2 ForProducing An Intermediate. However, the processes are not limited tosuch specific examples. ##STR68## (wherein R¹ represents a hydrogenatom, an alkyl group, a benzyl group or a phenyl group, R² and R³represent a hydrogen atom, an alkyl group, a halogen atom, a nitrogroup, an alkoxy group, a haloalkoxy group or a haloalkyl group, and Lrepresents a halogen atom.)

Namely, a compound represented by the formula V! is reacted with thecorresponding hydrazine derivative, for example, in DMSO, to obtain acompound represented by the formula VI!. Further, in concentratedhydrochloric acid, a diazonium salt is formed, and this is reacted withsulfurous acid gas in a solvent such as acetic acid in the presence ofcopper chloride to obtain a compound represented by the formula VII!.This is reacted with excess t-butylamine to produce a compoundrepresented by the formula I-d!. Then, the t-butyl group is removed withexcess trifluoroacetic acid to obtain an intermediate represented by theformula I-a!. ##STR69## (wherein R¹ represents an alkyl group, ahaloalkyl group, a benzyl group or a phenyl group, and R² and R³represent a hydrogen atom, an alkyl group, a halogen atom, an alkoxygroup, a phenyl group, a benzyl group or a haloalkoxy group.)

Namely, a compound represented by the formula IX! can be produced byreacting a compound represented by the formula VIII! with n-butyllithium, for example, in ethyl ether, within a temperature range of from-40° to -20° C., followed by blowing in sulfurous acid gas. Anintermediate represented by the formula II-a! can be produced by addingan aqueous solution of the compound represented by the formula IX! to anaqueous solution of a mixture of hydroxylamine-o-sulfonic acid and abase under cooling with ice.

In this reaction formula, the compound of the formula VIII! can beproduced by a method disclosed in a known literature such as LiebigsAnn. Chem., 908 (1980)!, Org. Synth. Coll. Vol. V, 650!, J. Chem. Soc.Perkin Trans. II, 1695, (1975)!, or Org. Synth, Coll. Vol. V, 941!.

The intermediate represented by the formula I-a! or II-a! can beproduced also by the following process. ##STR70## (wherein R¹ representsan alkyl group, a cycloalkyl group, a haloalkyl group, an alkoxyalkylgroup, a benzyloxyalkyl group, a benzyl group, a dialkylaminocarbonylgroup, an alkoxycarbonyl group, a alkylsulfonyl group, a phenylsulfonylgroup, a dialkylaminosulfonyl group, a haloalkylcarbonyl group, analkylcarbonyl group, a benzoyl group or an alkenyl group, R² or R³represents a hydrogen atom, a halogen atom, an alkoxy group, ahaloalkoxy group, a haloalkyl group, an alkoxycarbonyl group, a phenylgroup or a benzyl group, L represents a halogen atom, and M represents abromine atom or a chlorine atom.)

Namely, a compound represented by the formula X! is reacted withN-bromosuccinimide, N-chlorosuccinimide, or bromine or chlorine incarbon tetrachloride in the presence of a light and a radical reactioninitiating agent to obtain a compound represented by the formula XI!.The compound represented by the formula XI! is reacted with thiourea toobtain a compound represented by the formula XII!. The compoundrepresented by the formula XII! is reacted with chlorine or bromine in amixed solution of acetic acid and water to obtain a compound representedby the formula XIII!. Then, this compound is reacted with t-butylamineto obtain a compound represented by the formula XIV!. The compoundrepresented by the formula XIV! is reduced to obtain a compoundrepresented by the formula XV!. The compound represented by the formulaXV! and isoamylnitrous acid are reacted, followed by reaction withhydrochloric acid to obtain a compound represented by the formula XVI!.The compound represented by the formula XVI! is reacted with e.g. analkyl halide or a benzyl halide to obtain a compound represented by theformula I-d! or II-d!.

The compound represented by the formula XVI!, I-d! or II-d! can beconverted to a compound represented by the formula XVII! and anintermediate represented by the formula I-a! or II-a!, respectively, byremoving the t-butyl group with trifluoroacetic acid, as shown inProcess 1 For Producing An Intermediate.

Further, the compound represented by the formula XVII! is reacted withR¹ L (wherein R¹ and L have the same meanings as defined above) toobtain intermediates of the formulas I-a! and II-a!.

The intermediate represented by the formula I-a! may be prepared byvarious processes depending upon the types of the substituents. However,it can be produced by the processes represented by the following Process4 For Producing An Intermediate and Processes 5-1 to 5-3 For ProducingAn Intermediate. ##STR71## (wherein R¹ represents a hydrogen atom, analkyl group, a benzyl group or a phenyl group, R² represents a halogenatom, preferably a fluorine atom, R³ has the same meaning as definedabove, and R⁴ represents an alkoxy group, an alkoxyalkoxy group, abenzyloxy group, a cycloalkylalkoxy group, a haloalkoxy group, adialkylaminoalkoxy group, an alkylthio group, an alkylamino group, adialkylamino group or a benzylamino group.)

Namely, in this reaction, an intermediate represented by the formulaI-a! or II-a! is reacted with a compound represented by the formula R⁴-H (wherein R⁴ has the same meaning as defined above) in a polar solventsuch as DMSO, DMF, DMAC or NMP in the presence of a base such as sodiumhydride, potassium hydride, potassium carbonate, potassium t-butoxide,sodium hydroxide or potassium hydroxide, to obtain an intermediaterepresented by the formula I-e! or II-e!, respectively. ##STR72##(wherein R¹ represents an alkyl group, a benzyl group or a phenyl group,R³ has the same meaning as defined above, R⁵ represents an alkyl group,a benzyl group, an alkenyl group, an alkynyl group, a haloalkenyl group,a haloalkyl group, an alkoxyalkyl group, an alkoxycarbonylalkyl group ora cyanoalkyl group, and L¹ represents a halogen atom, analkylsulfonyloxy group, a haloalkylsulfonyloxy group or abenzenesulfonyloxy group which may be substituted.)

Namely, in this reaction formula, an intermediate represented by theformula I-f! or II-f! is reacted with a compound represented by theformula R⁵ -L¹ (wherein R⁵ and L¹ have the same meanings as definedabove) in a suitable solvent in the presence of a base, to obtain anintermediate represented by the formula I-g! or II-g!, respectively.

The intermediate represented by the formula I-f! or II-f! can beproduced by the following process. ##STR73## (wherein R¹ represents analkyl group, a benzyl group or a phenyl group, R² represents a halogenatom, preferably a fluorine atom, R³ represents a hydrogen atom, ahalogen atom, an alkyl group, a haloalkyl group, a haloalkoxy group oran alkoxy group, and R⁸ represents an alkyl group, a benzyl group or acycloalkyl group, preferably a cyclopropylmethyl group.)

Namely, in this reaction formula, an intermediate represented by theformula I-a! or II-a! is reacted with a compound of the formula R⁸ --OH(wherein R⁸ has the same meaning as defined above) in a suitable solventin the presence of a base, to obtain an intermediate represented by theformula I-h! or II-h!, which is further subjected to removal of theprotecting group to obtain an intermediate of the formula I-f! or II-f!,respectively. ##STR74## (wherein R¹ represents an alkyl group, a benzylgroup or a phenyl group, and R³ and R⁵ have the same meanings as definedabove.)

Namely, in this reaction formula, an intermediate represented by theformula I-f! or II-f! is subjected to a Mitsunobu reaction (as disclosedin Organic Reactions Vol. 42, p-335) using a compound represented by theformula R⁵ --OH (wherein R⁵ has the same meaning as defined above) in asuitable solvent, to obtain an intermediate of the formula I-g! orII-g!, respectively. ##STR75## (wherein R¹ represents an alkyl group, abenzyl group or a phenyl group, R³, R⁵ and L¹ have the same meanings asdefined above, and R⁶ represents an alkyl group, preferably a methylgroup.)

Namely, in this reaction formula, an intermediate represented by theformula I-f! or II-f! is reacted with acetal of DMF to obtain a compoundrepresented by the formula I-i! or II-i!, which is then reacted with acompound represented by the formula R⁵ -L¹ (wherein R⁵ and L¹ have thesame meanings as defined above) in a suitable solvent in the presence ofa base to obtain a compound represented by the formula I-j! or II-j!,which is then hydrolyzed with an acid or alkali to obtain anintermediate represented by the formula I-g! or II-g!.

Now, specific compounds of the intermediate represented by the formulaI-a! or II-a! will be listed in Table 3.

                  TABLE 3                                                         ______________________________________                                        Inter-                                                                        mediate                                                                       No.   R.sup.1                                                                              R.sup.2         R.sup.3 mp. (°C.)                         ______________________________________                                         ##STR76##                                                                    1     Me     Ph              H                                                2     Me     Bn              H                                                3     Me     SH              H                                                4     Me     SMe             H                                                5     Me     SEt             H       223-225                                  6     Me     SPr             H       208-209                                  7     Me     SO.sub.2 Me     H                                                8     Me     SO.sub.2 Et     H       271-273                                  9     Me     SOMe            H                                                10    Me     SO.sub.2 NHMe   H                                                11    Me     SO.sub.2 NHOMe  H                                                12    Me     SO.sub.2 NMe.sub.2                                                                            H       248-252                                  13    Me     SO.sub.2 NHBn   H                                                14    Me     SO.sub.2 NHPh   H                                                15    Me     SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                                H                                                16    Me     SO.sub.2 NHCH.sub.2 C CH                                                                      H                                                17    H      Cl              H       215-217                                  18    Me     Cl              H       268-270                                  19    Me     Cl              5-Cl    283-285                                  20    Et     Cl              H       180-182                                  21    Ph     Cl              H                                                22    Bn     Cl              H                                                23    Me     H               H       178-180                                  24    Me     F               H       221-223                                  25    Me     Br              H       285-287                                  26    Me     Me              H                                                27    Me     CN              H       274-281                                  28    Me     CF.sub.3        H                                                29    Me     H               5-Cl                                             30    Me     H               6-Cl                                             31    Me     H               7-Cl                                             32    Me     COH             H                                                33    Me     COMe            H                                                34    Me     COEt            H                                                35    Me     COPh            H                                                36    Me     CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H                                                37    Me     CO.sub.2 CH.sub.2 C CH                                                                        H                                                38    Me     COBn            H                                                39    Me     NO.sub.2        H       249-251                                  40    Me     NH.sub.2        H                                                41    Me     NHMe            H                                                42    Me     NMe.sub.2       H                                                43    Me     NHCOMe          H                                                44    Me     NHCOPh          H                                                45    Me     NHCOCH.sub.2 Cl H                                                46    Me     NHSO.sub.2 CH.sub.3                                                                           H                                                47    Me     NHSO.sub.2 Ph   H                                                48    Me     CO.sub.2 H      H                                                49    Me     CO.sub.2 Me     H       233-234                                  50    Me     CO.sub.2 Et     H       193-195                                  51    Me     CO.sub.2 Pr     H       185-188                                  52    Me     CO.sub.2 Pr-i   H       219-220                                  53    Me     CO.sub.2 Bu     H       167-168                                  54    Me     CO.sub.2 Pen    H                                                55    Me     CO.sub.2 Bn     H                                                56    Me     CO.sub.2 Ph     H                                                57    Me     CO.sub.2 CH.sub.2 CH.sub.2 F                                                                  H                                                58    Me     CO.sub.2 Me     5-F                                              59    Et     CO.sub.2 Me     H                                                60    Bu     CO.sub.2 Me     H                                                61    Bn     CO.sub.2 Me     H                                                62    Ph     CO.sub.2 Me     H                                                63    H      CO.sub.2 Et     H                                                64    Me     OH              H                                                65    Me     OMe             H       268-270                                  66    Me     OEt             H       230-233                                  67    Me     OPr             H       210-212                                  68    Me     OPr-i           H       200-201                                  69    Me     OBu             H       203-205                                  70    Me     OBn             H                                                71    Me     OBn(4-Cl)       H                                                72    Me     OBn(3-OMe)      H                                                73    Me     OBn(2-Me)       H                                                74    Me     OPh             H                                                75    Me     OPh(4-Cl)       H                                                76    Me     OPh(3-OMe)      H                                                77    Me     OPh(2-Me)       H                                                78    Me     OCH.sub.2 CHCH.sub.2                                                                          H                                                79    Me     OCH.sub.2 C CH  H                                                80    Me     OCH.sub.2 CF.sub.3                                                                            H                                                81    Me     OCH.sub.2 CH.sub.2 OMe                                                                        H                                                82    Me     OCH.sub.2 CH.sub.2 OPh                                                                        H                                                83    Me     OCOMe           H                                                84    Me     CONH.sub.2      H                                                85    Me     CONHMe          H                                                86    Me     CONHEt          H                                                87    Me     CONHPr          H                                                88    Me     CONMe.sub.2     H       274-275                                  89    Me     CONEt.sub.2     H                                                90    Me     CONHBn          H                                                91    Me     CONHPh          H                                                92    Me     CONHCH.sub.2 CHCH.sub.2                                                                       H                                                93    Me     CONHCH.sub.2 C CH                                                                             H                                                94    Me     CONHOMe         H                                                95    Me     H               5-F                                              96    Me     SO.sub.2 NH.sub.2                                                                             H                                                97    Me     SPr-i           H       228-231                                  98    Me     OCH.sub.2 CH.sub.2 OEt                                                                        H                                                99    Me     OCH.sub.2 CH.sub.2 OPr-i                                                                      H                                                100   Me     OCH.sub.2 CH.sub.2 OBu                                                                        H                                                101   Me     OCH.sub.2 CH.sub.2 OBu-t                                                                      H                                                102   Me     OCH.sub.2 CH.sub.2 NMe.sub.2                                                                  H                                                103   Me     OCH.sub.2 COOEt H                                                104   Me     OCH.sub.2 CH.sub.2 Cl                                                                         H                                                105   Me     OCH.sub.2 CH.sub.2 F                                                                          H                                                106   Me     OCH.sub.2 OCH.sub.3                                                                           H                                                167   Me     OCH(CF.sub.3)Me H                                                108   Me     H               5-OMe                                            109   Me     H               5-OEt                                            110   Me     H               5-OPr                                            111   Et     CO.sub.2 Me     H                                                112   Et     Br              H                                                113   Me     OCHF.sub.2      H                                                114   Me     SO.sub.2 Pr     H       270-272                                  115   Me     SO.sub.2 Pr-i   H       260-263                                  116   Me     SO.sub.2 Bu     H       287-290                                  117   Me     SBu             H       187-189                                  118   Me     OMe             5-Cl                                             119   Me     NHBn            H                                                120   Me     OCH.sub.2 Bu-t  H                                                121   Me     OCH.sub.2 CHF.sub.2                                                                           H                                                122   H      NO.sub.2        H       >300                                     123   H      Br              H       183-186                                  124   H      COOCH.sub.3     H       243-247                                  125   Me     H               5-CO.sub.2 Me                                                                         238-241                                   ##STR77##                                                                    126   Me     Ph              H                                                127   Me     Bn              H                                                128   Me     SH              H                                                129   Me     SMe             H                                                130   Me     SEt             H       145-147                                  131   Me     SPr             H                                                132   Me     SO.sub.2 Me     H                                                133   Me     SO.sub.2 Et     H       167-169                                  134   Me     SOMe            H                                                135   Me     SO.sub.2 NHMe   H                                                136   Me     SO.sub.2 NHOMe  H                                                137   Me     SO.sub.2 NMe.sub.2                                                                            H       218-220                                  138   Me     SO.sub.2 NHBn   H                                                139   Me     SO.sub.2 NHPh   H                                                140   Me     SO.sub.2 NHCH.sub.2 CHCH.sub.2                                                                H                                                141   Me     SO.sub.2 NHCH.sub.2 C CH                                                                      H                                                142   H      Cl              H       215-217                                  143   Me     Cl              H       173-175                                  144   Me     Cl              5-Cl                                             145   Et     Cl              H       182-184                                  146   Ph     Cl              H       220-221                                  147   Bn     Cl              H                                                148   Me     H               H       181-183                                  149   Me     F               H       151-152                                  150   Me     Br              H       182-183                                  151   Me     Me              H       149-151                                  152   Me     CN              H       227-228                                  153   Me     CF.sub.3        H                                                154   Me     H               5-Cl    186-188                                  155   Me     H               6-Cl    206-207                                  156   Me     H               7-Cl    175-177                                  157   Me     COH             H                                                158   Me     COMe            H                                                159   Me     COEt            H                                                160   Me     COPh            H                                                161   Me     CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  H                                                162   Me     CO.sub.2 CH.sub.2 C CH                                                                        H                                                163   Me     COBn            H                                                164   Me     NO.sub.2        H       193-194                                  165   Me     NH.sub.2        H                                                166   Me     NHMe            H       179-181                                  167   Me     NMe.sub.2       H       197-200                                  168   Me     NHCOMe          H                                                169   Me     NHCOPh          H                                                170   Me     NHCOCH.sub.2 Cl H                                                171   Me     NHSO.sub.2 CH.sub.3                                                                           H                                                172   Me     NHSO.sub.2 Ph   H                                                173   Me     CO.sub.2 H      H                                                174   Me     CO.sub.2 Me     H       160-163                                  175   Me     CO.sub.2 Et     H       135-137                                  176   Me     CO.sub.2 Pr     H       130-132                                  177   Me     CO.sub.2 Pr-i   H       145-147                                  178   Me     CO.sub.2 Bu     H       113-114                                  179   Me     CO.sub.2 Pen    H                                                180   Me     CO.sub.2 Bn     H                                                181   Me     CO.sub.2 Ph     H                                                182   Me     CO.sub.2 CH.sub.2 CH.sub.2 F                                                                  H                                                183   Me     CO.sub.2 Me     5-F                                              184   Et     CO.sub.2 Me     H                                                185   Bu     CO.sub.2 Me     H                                                186   Bn     CO.sub.2 Me     H                                                187   Ph     CO.sub.2 Me     H                                                188   H      CO.sub.2 Et     H                                                189   Me     OH              H       180-181                                  190   Me     OMe             H       265-268                                  191   Me     OEt             H       184-185                                  192   Me     OPr             H       186-188                                  193   Me     OPr-i           H       205-206                                  194   Me     OBu             H       152-154                                  195   Me     OBn             H                                                196   Me     OBn(4-Cl)       H                                                197   Me     OBn(3-OMe)      H                                                198   Me     OBn(2-Me)       H                                                199   Me     OPh             H                                                200   Me     OPh(4-Cl)       H                                                201   Me     OPh(3-OMe)      H                                                202   Me     OPh(2-Me)       H                                                203   Me     OCH.sub.2 CHCH.sub.2                                                                          H       143-144                                  204   Me     OCH.sub.2 C CH  H       180-181                                  205   Me     OCH.sub.2 CF.sub.3                                                                            H       182-183                                  206   Me     OCH.sub.2 CH.sub.2 OMe                                                                        H       174-176                                  207   Me     OCH.sub.2 CH.sub.2 OPh                                                                        H                                                208   Me     OCOMe           H                                                209   Me     CONH.sub.2      H                                                210   Me     CONHMe          H                                                211   Me     CONHEt          H                                                212   Me     CONHPr          H                                                213   Me     CONMe.sub.2     H       267-270                                  214   Me     CONHEt.sub.2    H                                                215   Me     CONHBn          H                                                216   Me     CONHPh          H                                                217   Me     CONHCH.sub.2 CHCH.sub.2                                                                       H                                                218   Me     CONHCH.sub.2 C CH                                                                             H                                                219   Me     CONHOMe         H                                                220   Me     H               5-F     174-175                                  221   Me     SO.sub.2 NH.sub.2                                                                             H                                                222   Me     SPr-i           H       134-135                                  223   Me     OCH.sub.2 CH.sub.2 OEt                                                                        H       116-120                                  224   Me     OCH.sub.2 CH.sub.2 OPr-i                                                                      H       118-119                                  225   Me     OCH.sub.2 CH.sub.2 OBu                                                                        H       144-145                                  226   Me     OCH.sub.2 CH.sub.2 OBu-t                                                                      H       183-184                                  227   Me     OCH.sub.2 CH.sub.2 NMe.sub.2                                                                  H       184-187                                  228   Me     OCH.sub.2 COOEt H       116-120                                  229   Me     OCH.sub.2 CH.sub.2 Cl                                                                         H       177-179                                  230   Me     OCH.sub.2 CH.sub.2 F                                                                          H       178-180                                  231   Me     OCH.sub.2 OCH.sub.3                                                                           H       163-165                                  232   Me     OCH(CF.sub.3)Me H       165-167                                  233   Me     H               5-OMe   169-172                                  234   Me     H               5-OEt   152-153                                  235   Me     H               5-OPr   149-151                                  236   Et     CO.sub.2 Me     H       123-125                                  237   Et     Br              H                                                238   Me     OCHF.sub.2      H       164-166                                  239   Me     SO.sub.2 Pr     H       176-178                                  240   Me     SO.sub.2 Pr-i   H       220-221                                  241   Me     SO.sub.2 Bu     H       156-158                                  242   Me     SBu             H       162-164                                  243   Me     OMe             5-Cl    161-163                                  244   Me     NHBn            H       189-191                                  245   Me     OCH.sub.2 Bu-t  H       207-208                                  246   Me     OCH.sub.2 CHF.sub.2                                                                           H       186-188                                  247   Me     OCH.sub.2 CH.sub.2 CH.sub.2 F                                                                 H       139-140                                  248   Me     OMe             H       138-140                                  249   Me     Cl              H       176-178                                  250   Me     OCH.sub.2 OEt   H       148-150                                  251   Me     OCH.sub.2 C(CH.sub.3)CH.sub.2                                                                 H       132-134                                  252   Me     OCH.sub.2 CHC(Me).sub.2                                                                       H       141-143                                  253   Me     OCH.sub.2 CHCHCl                                                                              H       164-166                                  254   Me                                                                                    ##STR78##      H       139-141                                  255   Me     OCH.sub.2 OBn   H       156-158                                  ______________________________________                                    

BEST MODE FOR CARRYING OUT THE INVENTION

Now, the present invention will be specifically explained by describingthe process for producing the intermediate and the process for producingthe compound of the present invention as Preparation Examples.

PREPARATION EXAMPLE 1 Preparation of1-methyl-4-fluoro-1H-indazole-3-sulfonamide (Intermediate No. 24)

75 g (539 mmol) of 2,6-difluorobenzonitrile was added to 300 ml of DMSO,and 33 g (716 mmol) of methylhydrazine was dropwise added thereto withstirring. The reaction proceeded exothermically, and the dropwiseaddition was continued while maintaining the temperature at a level offrom 80° to 100° C. After returning to room temperature, the mixture waspoured into a large excess amount of cool water, whereupon crystals werecollected by filtration and dried in air to obtain 72 g (yield: 81%) of3-amino-1-methyl-4-fluoro-1H-indazole (compound represented by theformula VI! (slightly yellow crystals).

Then, 70 g (424 mmol) of 3-amino-1-methyl-4-fluoro-1H-indazole wasdissolved in 200 ml of acetic acid, and 140 ml of concentratedhydrochloric acid was added thereto. The mixture was vigorously stirred,and a solution having 33 g (478 mmol) of sodium nitrite dissolved in 60ml of water, was gradually dropwise added thereto within a range of from-5° to -10° C. The diazonium salt solution thus obtained, was graduallydropwise added to a mixture having 17 g (100 mmol) of cupric chloridedihydrate added to a solution obtained by blowing sulfurous acid gasinto 370 ml of acetic acid until saturation (120 g). After completion ofthe dropwise addition, stirring was continued for one hour at atemperature of not higher than 0° C., and then the mixture was pouredinto a large excess amount of cold water, whereupon crystals werecollected by filtration and dried in air to obtain 70 g (yield: 66%) of1-methyl-4-fluoro-1H-indazole-3-sulfonylchloride (compound representedby the formula VII!) (slightly purple crystals).

Further, 13.9 g (56 mmol) of1-methyl-4-fluoro-1H-indazole-3-sulfonylchloride in 50 ml of THF, wasadded to 12.9 g (177 mmol) of t-butylamine in 100 ml of THF, and themixture was stirred at room temperature overnight. After completion ofthe reaction, the mixture was poured into a large excess amount ofwater, whereupon the crystals were collected by filtration and dried inair to obtain 15.9 g (yield: 99.6%) of3-(N-t-butylsulfamoyl)-1-methyl-4-fluoro-1H-indazole (compoundrepresented by the formula I-d!) (slightly purple crystals).

15 g (53 mmol) of 3-(N-t-butylsulfamoyl)-1-methyl-4-fluoro-1H-indazolewas added to 50 ml of trifluoroacetic acid, and the mixture was stirredovernight. After completion of the reaction, trifluoroacetic acid wasdistilled off under reduced pressure, and the residue was washed withn-hexane to obtain 10.5 g (yield: 86.8%) of1-methyl-4-fluoro-1H-indazole-3-sulfonamide (slightly purple crystals).Melting point: 221°-223° C.

PREPARATION EXAMPLE 2 Preparation of1-(1-methyl-4-fluoro-1H-indazole-3-sulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea(Compound No. I-26)

0.35 g (2.3 mmol) of DBU was added to a solution containing 0.5 g (2.3mmol) of 1-methyl-4-fluoro-1H-indazole-3-sulfonamide obtained inPreparation Example 1 and 0.62 g (2.3 mmol) of phenyl(4,6-dimethoxypyrimidin-2-yl)carbamate in 20 ml of acetonitrile, and themixture was stirred at room temperature for 12 hours. The mixture waspoured into ice water and acidified with citric acid, whereupon theformed crystals were collected by filtration and washed with ice water,IPE and ethyl ether to obtain 0.49 g (yield: 52%) of the desired product(colorless needle like crystals). Melting point: 205°-209° C.

PREPARATION EXAMPLE 3-1 Preparation of methyl2-bromomethyl-3-nitrobenzoate (Compound Represented by the Formula XI!)

A suspension containing 98 g (0.5 mol) of methyl2-methyl-3-nitrobenzoate, 100 g (0.56 mol) of N-bromosuccinimide and 1 gof benzoyl peroxide in carbon tetrachloride (800 ml), was refluxed for 3days under irradiation with 500 W. The suspension was cooled to roomtemperature and subjected to filtration, whereupon the filtrate wasconcentrated. To the residue, ethyl ether (200 ml) and IPE (200 ml) wereadded, whereupon the formed crystals were collected by filtration toobtain 121 g (yield: 88.3%) of the desired product. Melting point:65°-67° C.

PREPARATION EXAMPLE 3-2 Preparation ofS-(2-methoxycarbonyl-6-nitrobenzyl)-thiouronium bromide (CompoundRepresented by the Formula XII!

In methanol (2 l), 207 g (0.76 mol) of the product from PreparationExample 3-1 and 57.6 g (0.76 mol) of thiourea were refluxed for 12hours. After cooling, methanol was distilled off, and ethyl acetate (1l) was added to the residue. The product was subjected to filtration.This product was used for the subsequent reaction without purification.The obtained amount: 246 g (yield: 93%)

PREPARATION EXAMPLE 3-3 Preparation of methyl2-(t-butylaminosulfonylmethyl)-3-nitrobenzoate (Compounds Represented bythe Formulas XIII! and XIV!)

110 g (0.32 mol) of the product from Preparation Example 3-2 in water (2l) and acetic acid (1 l), was cooled to 5° C. and chlorine was blownthereto for 4 hours at a temperature of from 5° to 10° C. And, themixture was stirred at room temperature for one hour. Then, the productwas collected by filtration and washed with ice water and then dissolvedin 1 l of dichloromethane. To this solution, 54 g (0.74 mol) oft-butylamine was dropwise added at a temperature of from 0° to 5° C.Then, the mixture was stirred at room temperature for 2 hours. Theorganic layer was washed with water and then concentrated. IPE was addedto the residue, followed by filtration to obtain 63 g (yield: 60.1%) ofthe desired product. This product was used for the subsequent reactionwithout purification.

PREPARATION EXAMPLE 3-4 Preparation of methyl3-amino-2-(t-butylaminosulfonylmethyl)benzoate (Compound Represented bythe Formula XV!)

A solution containing 48 g (0.145 mol) of the product from PreparationExample 3-3 and 164 g (0.73 mol) of stannous chloride dihydrate in 300ml of ethanol, was refluxed for 2 hours. After cooling, it was added to2 l of ethyl acetate, and powdery sodium hydrogencarbonate (500 g) wasgradually added thereto. The formed salt was collected by filtration andthoroughly washed with ethyl acetate. The organic layer was concentratedto obtain 35.9 g (yield: 82.4%) of the desired product. Melting point:123°-125° C.

PREPARATION EXAMPLE 3-5 Preparation of methyl3-(t-butylaminosulfonyl)-1H-indazole-4-carboxylate (Compound Representedby the Formula XVI!)

A suspension containing 30 g (0.1 mol) from Preparation Example 3-4,30.6 g (0.3 mol) of acetic anhydride and 10 g (0.102 mol) of potassiumacetate in benzene (500 ml), was heated to 80° C., and at the sametemperature, 17.6 g (0.15 mol) of isoamyl nitrite was dropwise addedthereto. Further, the mixture was refluxed for 12 hours and then cooled,and the salt was filtered. The organic layer was concentrated, andmethanol (500 ml) and 10% hydrochloric acid (20 ml) were added to theresidue, and the mixture was refluxed for one hour. After distilling offmethanol, water was added thereto, and the mixture was neutralized withan aqueous sodium hydrogencarbonate solution. The formed crystals werecollected by filtration to obtain 29.3 g (yield: 94.1%) of the desiredproduct. Melting point: 218°-220° C.

PREPARATION EXAMPLE 3-6 Preparation of methyl3-(t-butylaminosulfonyl)-1-methyl-1H-indazole-4-carboxylate and methyl3-(t-butylaminosulfonyl) 2-methyl-2H-indazole-4-carboxylate (CompoundsRepresented by the Formulas I-d! and II-d!)

6.8 g (48 mmol) of methyl iodide was added to a solution containing 10 g(32 mmol) of the product from Preparation Example 3-5 and 6.6 g (48mmol) of potassium carbonate in methanol (200 ml), and the mixture wasrefluxed for 3 hours. Methanol was distilled off, and water was added tothe residue, and the mixture was extracted with ethyl acetate. Theorganic layer was washed with water, dried over anhydrous magnesiumsulfate, then concentrated and purified by silica gel columnchromatography to obtain 5.9 g (yield; 56.8%; melting point: 189°-190°C.) of methyl3-(t-butylaminosulfonyl)-1-methyl-1H-indazole-4-carboxylate and 2.1 g(yield: 19.8%; melting point: 147°-148° C.) of methyl3-(t-butylaminosulfonyl) 2-methyl-2H-indazole-4-carboxylate.

PREPARATION EXAMPLE 4 Preparation of 2-methyl-2H-indazole-3-sulfonamide(Intermediate No. 148)

A solution containing 9.5 g (72 mmol) of 2-methyl-2H-indazole in 200 mlof ethyl ether, was cooled to -30° C., and 61.4 g (144 mmol) of n-butyllithium (a 15% hexane solution) was dropwise added thereto. The mixturewas stirred for one hour at the same temperature, and then an excessamount of sulfurous acid gas was blown thereinto for 3 hours at atemperature of not higher than -20° C. After completion of the reaction,the mixture was returned to room temperature, stirred for 12 hours andthen diluted with ethyl ether. The product was subjected to filtration.The crystals were dried to obtain crude lithium2-methyl-2H-indazole-3-sulfinate. This product was used for thesubsequent reaction without purification. 48.8 g (430 mmol) ofhydroxylamine-O-sulfonic acid was gradually added to a solutioncontaining 17.2 g (430 mmol) of sodium hydroxide in water (300 ml) undercooling with ice (not higher than 10° C.). This solution was added allat once to a solution containing the crude lithium2-methyl-2H-indazole-3-sulfinate previously prepared in water (100 ml),and then the mixture was stirred for 12 hours at room temperature.Formed crystals were collected by filtration to obtain 8.8 g (yield:58%) of 2-methyl-2H-indazole-3-sulfonamide (slightly yellow granularcrystals). Melting point: 181°-183° C.

PREPARATION EXAMPLE 5 Preparation of1-(2-methyl-2H-indazole-3-sulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea(Compound No. II-23)

2.3 g (15 mmol) of DBU was added to a solution containing 3.2 g (15mmol) of 2-methyl-2H-indazole-3-sulfonamide obtained in PreparationExample 4 and 4.1 g (15 mmol) of phenyl(4,6-dimethoxypyrimidin-2-yl)carbamate in acetonitrile (50 ml), and themixture was stirred at room temperature for 12 hours. The mixture waspoured into ice water and acidified with citric acid. Formed crystalswere collected by filtration and washed with ice water, IPE and ethylether, to obtain 4.0 g (yield: 68%) of the desired product (colorlessneedle like crystals). Melting point: 199°-202° C.

PREPARATION EXAMPLE 6 Preparation of4-methoxy-1-methyl-1H-indazole-3-sulfonamide (Intermediate No. 65)

A solution containing 5 g (21.8 mmol) of4-fluoro-1-methyl-1H-indazole-3-sulfonamide and 12.6 g of sodiummethoxide (a 28% methanol solution) (65 mmol) in DMSO (50 ml), wasstirred at 130° C. for one hour. After confirming the disappearance ofthe starting material by thin layer chromatography (TLC), the mixturewas poured into ice water and acidified with citric acid. Formedcrystals were collected by filtration and washed with water and IPE toobtain 3.2 g (yield: 60.9%) of the desired product. Melting point:268°-270° C.

PREPARATION EXAMPLE 7 Preparation of4-ethylthio-2-methyl-2H-indazole-3-sulfonamide (Intermediate-No. 130)

4.8 g (77 mmol) of ethanethiol was added to a solution containing 8.6 g(77 mmol) of potassium t-butoxide in DMSO (70 ml), under cooling withice, and 8 g (35 mmol) of 4-fluoro-2-methyl-2H-indazole-3-sulfonamidewas further added thereto. This mixture was stirred at 120° C. for 2hours. After confirming the disappearance of the starting material byTLC, treatment was conducted in the same manner as in PreparationExample 6 to obtain 6.8 g (yield: 72.5%) of the desired product.Melting: 145°-147° C.

PREPARATION EXAMPLE 8-1 Preparation of4-cyclopropylmethoxy-2-methyl-2H-indazole-3-sulfonamide (IntermediateNo. 254)

2.8 g (70 mmol) of 60% sodium hydride was suspended in 50 ml of DMSO,and 6 g (83 mmol) of cyclopropane methanol was dropwise added thereto.The mixture was stirred at room temperature for one hour, and then 5.4 g(24 mmol) of ⁴ -fluoro-² -methyl-2H-indazole-3-sulfonamide was addedthereto. The mixture was stirred at 130° C. for 3 hours. After thereaction, the mixture was poured into ice water, acidified with citricacid and extracted with ethyl acetate. The organic layer was washed withwater and then concentrated. Formed crystals were collected byfiltration, washed with IPE and then dried to obtain 5.8 g (yield: 90%)of the desired product. Melting point: 139°-141° C.

PREPARATION EXAMPLE 8-2 Preparation of4-hydroxy-2-methyl-2H-indazole-3-sulfonamide (Intermediate No. 189)

A mixture comprising 62 g (221 mmol) of4-cyclopropylmethoxy-2-methyl-2H-indazole-3-sulfonamide, 120 ml ofacetic acid and 120 ml of concentrated hydrochloric acid, was stirred at80° C. for one hour. After concentrating acetic acid-hydrochloric acid,the mixture was poured into ice water. Crystals were collected byfiltration and washed with water. Further, the crystals were washed withIPE and dried to obtain 35.1 g (yield: 70%) of the desired product.Melting point: 180°-181° C.

PREPARATION EXAMPLE 8-3 Preparation of4-allyloxy-2-methyl-2H-indazole-3-sulfonamide (Intermediate No. 203)

1.3 g of allyl bromide was added to a mixture comprising 5 g (22 mmol)of 4-hydroxy-2-methyl-2H-indazole-3-sulfonamide and 50 ml of a DMFsolution of 1.9 g (22 mmol) of sodium hydrogencarbonate, and the mixturewas stirred at room temperature for 12 hours. The mixture was pouredinto ice water, acidified with citric acid and extracted with ethylacetate. The organic layer was washed, then concentrated and purified bycolumn chromatography (hexane/ethyl acetate=2/1) to obtain 1.9 g (yield:32.5%) of the desired product. Melting point: 143°-144° C.

PREPARATION EXAMPLE 9 Preparation of4-(2-chloroethoxy-2-methyl-2H-indazole-3-sulfonamide (Intermediate No.229) (Mitsunobu Reaction)

3.8 g (22 mmol) of diethylazo dicarboxylate was added to a solutioncontaining 5 g (22 mmol) of4-hydroxy-2-methyl-2H-indazole-3-sulfonamide, 1.8 g (22 mmol) of2-chloroethanol and 5.8 g (22 mmol) of triphenylphosphine in 50 ml ofTHF, and the mixture was stirred at room temperature for 20 hours. Themixture was poured into water and extracted with ethyl acetate. Theorganic layer was washed with water, then concentrated and purified bycolumn chromatography (hexane/ethyl acetate=2/1) to obtain 1.66 g(yield: 26%) of the desired product. Melting point: 177°-179° C.

PREPARATION EXAMPLE 10-1 Preparation of N¹,N¹ -dimethyl-N² -(4-hydroxy-2-methyl-2H-indazol-3-yl)sulfonyl!formamidine (CompoundRepresented by the Formula II-i!)

21.3 g (174 mmol) of dimethylformamide dimethylacetal was dropwise addedto a solution containing 33 g (145 mmol) of ⁴-hydroxy-2-methyl-2H-indazole-3-sulfonamide in 200 ml of acetonitrile,at room temperature. The mixture was stirred for one hour, then pouredinto ice water and extracted with ethyl acetate. The organic layer waswashed with water, then concentrated and purified by columnchromatography to obtain 35.2 g (yield: 86.3%) of the desired product.Melting point: 118°-119° C.

PREPARATION EXAMPLE 10-2 Preparation of N¹,N¹ -dimethyl-N² -{4-(2-fluoroethoxy)-2-methyl-2H-indazol-3-yl!sulfonyl}formamidine(Compound Represented by the Formula II-j!)

4.2 g (15 mmol) of N¹,N¹ -dimethyl-N² -(4-hydroxy-2-methyl-2H-indazol-3-yl)sulfonyl!formamidine was added to asuspension containing 0.6 g (15 mmol) of 60% sodium hydride in 50 ml ofDMF, and the mixture was stirred at room temperature for one hour.Further, 2 g (16 mmol) of 1-bromo-2-fluoroethane was added thereto, andthe mixture was stirred at room temperature for 12 hours. The mixturewas poured into ice water, and the formed crystals were collected byfiltration and washed with water and IPE to obtain the desired product.This product was used for the subsequent reaction without purification.Obtained amount: 3.4 g (yield: 69.5%)

PREPARATION EXAMPLE 10-3 Preparation of4-(2-fluoroethoxy)-2-methyl-2H-indazole-3-sulfonamide (Intermediate No.230)

A mixture comprising 3.4 g of N¹,N¹ -dimethyl-N² -{4-(2-fluoroethoxy)-2-methyl-2H-indazol-3-yl!sulfonyl}formamidine, 5 mlof concentrated hydrochloric acid and 50 ml of ethanol, was refluxed for12 hours. Disappearance of the starting material was confirmed by TLC,and then ethanol was distilled off. Water was added to the residue,whereupon the formed crystals were collected by filtration and washedwith water and IPE to obtain 2.4 g (yield: 85%) of the desired product.Melting point: 178°-180° C.

PREPARATION EXAMPLE 11 Preparation of4-chloro-2-methyl-2H-indazole-3-sulfonamide (Intermediate No. 143)

36.1 g (0.24 mol) of 4-chloro-1H-indazole was added to a solutioncontaining 28.4 g (0.7 mol) of sodium hydroxide in 500 ml of methanol,and 85.2 g (0.6 mol) of methyl iodide was dropwise added thereto. Themixture was heated and refluxed for 4 hours. Then, methanol wasdistilled off, and water was added to the residue, followed byextraction with dichloromethane. The organic layer was washed withwater, dried and concentrated to obtain a mixture of4-chloro-1-methyl-1H-indazole and 4-chloro-2-methyl-2H-indazole. Thismixture was separated by silica gel column chromatography (ethylacetate/hexane=4/1) to obtain 17.4 g (yield: 43.6%) of4-chloro-2-methyl-2H-indazole (yellow liquid, refractive index (20° C.):1.6095).

A solution containing 16 g (0.1 mol) of 4-chloro-2-methyl-2H-indazole in300 ml of ethyl ether, was cooled to -30° C., and 85.4 g (0.2 mol) ofn-butyl lithium (15% hexane solution) was dropwise added thereto. Themixture was stirred for one hour at the same temperature. Then, anexcess amount of sulfurous acid gas was blown thereinto at a temperatureof not higher than -20° C. for 3 hours. After completion of thereaction, the mixture was returned to room temperature and diluted withethyl ether, and the product was subjected to filtration. Crystals weredried to obtain crude lithium 4-chloro-2-methyl-2H-indazole-3-sulfinate.This product was used for the subsequent reaction without purification.

45.2 g (0.4 mol) of hydroxylamine-O-sulfonic acid was gradually added toa solution containing 16 g (0.4 mol) of sodium hydroxide in water (300ml) under cooling with ice (<10° C.). This solution was added all atonce to a solution of the previously prepared crude lithium4-chloro-2-methyl-2H-indazole-3-sulfinate in water (100 ml). The mixturewas stirred at room temperature for 12 hours. Formed crystals werecollected by filtration to obtain 17.1 g (yield: 69.8%) of the desired4-chloro-2-methyl-2H-indazole-3-sulfonamide (slightly yellow granularcrystals). Melting point: 173°-175° C.

PREPARATION EXAMPLE 12 Preparation of1-(4-chloro-2-methyl-2H-indazole-3-sulfonyl)-3-(4,6-dimethoxypyrimidin-2-yl)urea(Compound No. II-134)

0.5 g (3.3 mmol) of DBU was added to a solution containing 0.8 g (3.3mmol) of 4-chloro-2-methyl-2H-indazole-3-sulfonamide obtained inPreparation Example 11 and 0.9 g (3.3 mmol) of phenyl(4,6-dimethoxypyrimidin-2-yl)carbamate in acetonitrile (50 ml), and themixture was stirred at room temperature for 12 hours. The mixture waspoured into ice water and acidified with citric acid. Formed crystalswere collected by filtration and sequentially washed with water,isopropyl ether and ethyl ether, to obtain 1.2 g (yield: 85%) of thedesired product (colorless needle-like crystals). Melting point:171°-172° C.

The herbicide of the present invention contains an indazolesulfonylureaderivative represented by the general formula I! or II! as an activeingredient.

For the compound of the present invention to be used as a herbicide, thecompound of the present invention may be used by itself. However, it maybe used in the form of a formulation such as a dust, a wettable powder,an emulsifiable concentrate, a microgranule or a granule by blending itwith a carrier, a surfactant, a dispersant or an adjuvant which iscommonly used for formulations.

The carrier to be used for such formulations, may, for example, be asolid carrier such as Zeeklite, talc, bentonite, clay, kaolin,diatomaceous earth, fine silica, vermiculite, calcium carbonate, slakedlime, silica sand, ammonium sulfate or urea, or a liquid carrier such asisopropyl alcohol, xylene, cyclohexane or methylnaphthalene.

As the surfactant and dispersant, a metal salt of alkylbenzenesulfonicacid, a metal salt of dinaphthylmethane disulfonic acid, a salt ofalcohol-sulfuric acid ester, an alkylaryl sulfonate, a lignin sulfonate,a polyoxyethylene glycol ether, a polyoxyethylene alkylaryl ether or apolyoxyethylene sorbitol monoalkylate may, for example, be mentioned.

The adjuvant may, for example, be carboxymethyl cellulose, polyethyleneglycol or gum arabic.

In practical use, the herbicide may be diluted to a suitableconcentration before application, or may be directly applied.

The herbicide of the present invention may be used for application tofoliage, soil or water surface. The blending proportion of the activeingredient is suitably selected as the case requires. However, in a caseof a dust or a granule, the proportion of the active ingredient isselected suitably within a range of from 0.01 to 10% (by weight),preferably from 0.05 to 5% (by weight). In a case of an emulsifiableconcentrate or a wettable powder, the proportion is selected suitablywithin a range of from 1 to 50% (by weight), preferably from 5 to 30%(by weight).

The dose of the herbicide of the present invention varies depending uponthe type of the compound, the weeds to be controlled, the germinationtendency, the environmental conditions and the type of the formulationto be used. However, in the case of a dust or a granule which is used byitself, the dose of the active ingredient is selected suitably within arange of from 0.1 g to 5 kg, preferably from 1 g to 1 kg, per 10 ares.In a case of an emulsifiable concentrate or a wettable powder which isused in a liquid state, the dose of the active ingredient is selectedsuitably within a range of from 0.1 to 50,000 ppm, preferably from 10 to10,000 ppm.

Further, the compound of the present invention may be used incombination with an insecticide, a fungicide, other herbicide, a plantgrowth controlling agent, a fertilizer or the like, as the caserequires.

Now, the formulation method will be described with reference to typicalFormulation Examples. The compounds, types of the additives and blendingratios are not limited to such specific Examples and may be changedwithin wide ranges. In the following description, "parts" means "partsby weight".

FORMULATION EXAMPLE 1 (Wettable Powder)

To 10 parts of Compound No. I-9 or II-26, 0.5 part ofpolyoxyethyleneoctylphenyl ether, 0.5 part of sodium β-naphthalenesulfonate-formalin condensate, 20 parts of diatomaceous earth and 69parts of clay were mixed and pulverized to obtain a wettable powder.

FORMULATION EXAMPLE 2 (Wettable Powder)

To 10 parts of Compound No. I-63 or II-134, 0.5 part ofpolyoxyethyleneoctylphenyl ether, 0.5 part of sodium β-naphthalenesulfonate-formalin condensate, 20 parts of diatomaceous earth, 5 partsof fine silica and 64 parts of clay were mixed and pulverized to obtaina wettable powder.

FORMULATION EXAMPLE 3 (Wettable Powder)

To 10 parts of Compound No. I-134 or II-104, 0.5 part ofpolyoxyethyleneoctylphenyl ether, 0.5 part of sodium β-naphthalenesulfonate-formalin condensate, 20 parts of diatomaceous earth, 5 partsof fine silica and 64 parts of calcium carbonate, were mixed andpulverized to obtain a wettable powder.

FORMULATION EXAMPLE 4 (Emulsifiable Concentrate)

To parts of Compound No. I-92 or II-64, 60 parts of a mixture comprisingequal amounts of xylene and isophorone and 10 parts of a mixturecomprising a polyoxyethylene sorbitol alkylate surfactant, apolyoxyethylenealkylaryl polymer and an alkylaryl sulfonate, were added,and the mixture was thoroughly stirred to obtain an emulsifiableconcentrate.

FORMULATION EXAMPLE 5 (Granule)

10 Parts of Compound No. I-64 or II-142, 80 parts of a bulking agentcomprising a 1:3 mixture of talc and bentonite, 5 parts of fine silica,5 parts of a mixture comprising a polyoxyethylene sorbitol alkylatesurfactant, a polyoxyethylenealkylaryl polymer and an alkylarylsulfonate and 10 parts of water were mixed and thoroughly kneaded toobtain a paste, which was extruded from sieve apertures with a diameterof 0.7 mm. The extruded product was dried and then cut into a length offrom 0.5 to 1 mm to obtain granules.

The compound of the present invention represented by the general formulaI! or II! is capable of controlling annual weeds such as barnyardgrass(Echinochloa oryzicola), smallflower umbrella-plant (Cyperus difformis)and monochoria (Monochoria vaginalis) as well as perennial weeds such asJapanese ribbon wapato (Sagittaria pygmaea), arrowhead (Sagittariatrifolia), water nutgrass (Cvperus serotinus), water chestnut(Eleocharis kuroquwai), bulrush (Scirpus juncoides) and narrow-leavedarrowhead (Alisma canaliculatum), which germinate in paddy fields.Further, it exhibits excellent herbicidal effects against various weedsproblematic in upland fields, including broadleaf weeds such assmartweed (Polygonum lapathifolium), green amaranth (Amaranthusviridis), lambsquater (Chenopodium album), goose grass (Galium aparine),chickweed (Stellaria media), velvetleaf (Abtilon theophrasti), pricklysida (Sida spinosa), hemp sesbania (Sesbania exaltata), morningglory(Ipomoea spp) and common cocklebur (Xanthium strumarium), perennial andannual syperaceous weeds such as purple nutsedge (Cyperus rotundus),yellow nutsedge (Cyperus esculentus), himekugu (Cyperus brevifolius var.leiolepis), annual sedge (Cyperus microiria) and rice flatsedge (Cyperusiria), and gramineous weeds such as barnyardgrass (Echinochloacrus-galli), goosegrass (Eleusine indica), greenfoxtail (Setariaviridis), annual bluegrass (Poa annua), johnsongrass (Sorghumhalepense), water foxtail (Alopecurus aegualis) and wild oat (Avenafatua), over a wide range from the preemergence stage to the growingstage.

On the other hand, the herbicide of the present invention is highly safeto crop plants and exhibits particularly high safety to e.g. rice,wheat, barley, corn, grain sorghum and sugar beat.

Now, the effects of the compounds of the present invention will bedescribed with reference to Test Examples.

TEST EXAMPLE 1 (Test on Herbicidal Effects by Paddy Field SoilTreatment)

In a plastic pot (surface area: 100 cm²) filled with paddy field soil,barnyardgrass (Ec), monochoria (Mo) and bulrush (Sc) were sown afterpuddling and leveling, and flooded to a water depth of 3 cm. Next day, awettable powder prepared in accordance with Formulation Example 1 wasdiluted with water and applied dropwise to the water surface. The dosewas 100 g of the active ingredient per 10 ares. The plants were thencultured in a green house, and the evaluation of the herbicidal effectswas conducted on the 21st day after the application in accordance withthe standards as identified in Table 4. The results are shown in Table5.

                  TABLE 4                                                         ______________________________________                                                      Herbicidal effects                                              Index         (growth-controlling degree)                                     No.           or phytotoxicity                                                ______________________________________                                        5             Herbicidal effect or phytotoxicity:                                           at least 90%                                                    4             Herbicidal effect or phytotoxicity:                                           at least 70% and less than 90%                                  3             Herbicidal effect or phytotoxicity:                                           at least 50% and less than 70%                                  2             Herbicidal effect or phytotoxicity:                                           at least 30% and less than 50%                                  1             Herbicidal effect or phytotoxicity:                                           at least 10 and less than 30%                                   0             Herbicidal effect or phytotoxicity:                                           0 to less than 10%                                              ______________________________________                                    

                  TABLE 5                                                         ______________________________________                                                   Herbicidal                                                         Compound   effects                                                            No.        Ec            Mo    Sc                                             ______________________________________                                        I-5        5             5     5                                              I-6        5             5     5                                              I-8        5             5     5                                              I-17       5             5     5                                              I-18       5             5     5                                              I-19       5             5     5                                              I-20       5             5     5                                              I-23       5             5     5                                              I-25       5             5     5                                              I-26       5             5     5                                              I-27       5             5     5                                              I-28       5             5     5                                              I-29       5             5     5                                              I-31       5             5     5                                              I-32       5             5     5                                              I-33       5             5     5                                              I-34       5             5     5                                              I-35       5             5     5                                              I-63       5             5     5                                              I-64       5             5     5                                              I-65       5             5     5                                              I-66       5             5     5                                              I-67       5             5     5                                              I-79       5             5     5                                              I-91       5             5     5                                              I-92       5             5     5                                              I-93       5             5     5                                              I-94       5             5     5                                              I-95       5             5     5                                              I-111      5             5     5                                              I-114      5             5     5                                              I-120      5             5     5                                              I-131      5             5     5                                              I-134      5             5     5                                              I-136      3             5     5                                              I-149      5             5     4                                              I-150      5             5     5                                              I-151      5             5     4                                              I-153      5             5     5                                              I-157      5             5     5                                              I-158      5             5     5                                              I-160      5             5     5                                              I-161      5             5     5                                              I-162      5             5     5                                              I-174      5             5     5                                              I-175      5             5     5                                              I-176      5             5     5                                              I-179      5             5     5                                              I-180      5             5     5                                              I-181      5             5     5                                              I-182      5             5     5                                              I-183      5             5     5                                              I-184      5             5     5                                              I-194      5             5     5                                              I-204      5             5     5                                              I-205      5             5     5                                              I-216      5             5     5                                              I-218      5             5     4                                              I-322      5             5     5                                              I-334      5             5     5                                              I-337      5             5     5                                              I-506      5             5     5                                              I-507      5             5     5                                              I-508      4             5     4                                              I-513      5             5     5                                              I-514      5             5     5                                              I-516      5             5     5                                              I-517      5             5     5                                              I-518      5             5     5                                              I-519      5             5     4                                              I-520      3             5     5                                              I-527      3             5     5                                              I-530      5             5     5                                              I-555      5             5     4                                              I-641      5             5     5                                              I-645      3             5     5                                              I-906      3             5     5                                              II-5       5             5     5                                              II-6       5             5     5                                              II-8       5             5     5                                              II-17      5             5     5                                              II-18      4             5     4                                              II-19      5             5     5                                              II-20      5             5     5                                              II-23      5             5     5                                              II-25      5             5     5                                              II-26      5             5     5                                              II-27      5             5     5                                              II-28      5             5     5                                              II-29      5             5     5                                              II-31      5             5     5                                              II-32      5             5     5                                              II-33      5             5     5                                              II-34      5             5     5                                              II-35      5             5     5                                              II-36      5             5     5                                              II-38      5             5     5                                              II-42      4             5     5                                              II-53      5             5     5                                              II-55      5             5     5                                              II-63      5             5     5                                              II-64      5             5     5                                              II-65      5             5     5                                              II-66      5             5     5                                              II-67      5             5     5                                              II-91      5             5     5                                              II-92      5             5     5                                              II-93      5             5     5                                              II-94      5             5     5                                              II-95      5             5     5                                              II-104     5             5     5                                              II-106     5             5     5                                              II-107     5             5     5                                              II-110     5             5     5                                              II-111     5             5     5                                              II-112     5             5     5                                              II-113     5             5     5                                              II-114     5             5     5                                              II-115     5             5     5                                              II-120     5             5     5                                              II-127     5             5     5                                              II-129     4             5     5                                              II-130     5             5     5                                              II-131     5             5     5                                              II-132     3             5     5                                              II-134     5             5     5                                              II-136     3             5     5                                              II-137     5             5     5                                              II-141     5             5     5                                              II-142     5             5     5                                              II-143     5             5     5                                              II-149     5             5     5                                              II-150     5             5     5                                              II-151     5             5     5                                              II-153     5             5     5                                              II-155     5             5     5                                              II-156     5             5     5                                              II-157     5             5     5                                              II-158     5             5     5                                              II-159     5             5     5                                              II-160     5             5     5                                              II-161     5             5     5                                              II-162     5             5     5                                              II-163     5             5     5                                              II-166     5             5     5                                              II-168     5             5     5                                              II-169     5             5     5                                              II-174     5             5     5                                              II-175     5             5     5                                              II-176     5             5     5                                              II-177     5             5     5                                              II-178     5             5     5                                              II-179     5             5     5                                              II-180     5             5     5                                              II-181     5             5     5                                              II-182     5             5     5                                              II-183     5             5     5                                              II-184     5             5     5                                              II-185     5             5     5                                              II-188     5             5     5                                              II-189     5             5     5                                              II-194     5             5     5                                              II-195     5             5     5                                              II-197     5             5     5                                              II-198     5             5     5                                              II-199     5             5     5                                              II-200     5             5     5                                              II-202     4             5     5                                              II-204     5             5     5                                              II-208     5             5     5                                              II-215     5             5     5                                              II-220     5             5     5                                              II-225     5             5     5                                              II-227     5             5     5                                              II-531     5             5     5                                              ______________________________________                                    

TEST EXAMPLE 2 (Test on Herbicidal Effects by Upland Field SoilTreatment)

In a plastic pot (surface area: 120 cm²) filled with upland field soil,pale smartweed (Po), slender amaranth (Am), common lambsquarters (Ch)and rice flatsedge (Ci) were sown and covered with soil. A wettablepowder prepared in accordance with Formulation Example 1 was dilutedwith water and applied uniformly to the soil surface by a small-sizedsprayer in an amount of 100 l/10 ares so as to apply 100 g of the activeingredient per 10 ares. The plants were then cultured in a green house,and the evaluation of the herbicidal effects was conducted on the 21stday after the application in accordance with the standards as identifiedin Table 4. The results are shown in Table

                  TABLE 6                                                         ______________________________________                                                    Herbicidal                                                        Compound    effects                                                           No.         Po    Am           Ch  Ci                                         ______________________________________                                        I-5         5     5            5   5                                          I-6         5     5            5   5                                          I-8         5     5            5   5                                          I-17        5     5            5   5                                          I-18        5     5            5   5                                          I-19        5     5            5   5                                          I-20        5     5            5   5                                          I-23        5     5            5   --                                         I-25        5     5            5   --                                         I-26        5     5            5   5                                          I-27        5     5            5   5                                          I-28        5     5            5   --                                         I-29        5     5            5   --                                         I-31        5     5            5   5                                          I-32        5     5            5   5                                          I-33        5     5            5   5                                          I-34        5     5            5   5                                          I-35        5     5            5   5                                          I-53        5     5            5   5                                          I-63        5     5            5   5                                          I-64        5     5            5   5                                          I-65        5     5            5   5                                          I-66        5     5            5   5                                          I-67        5     5            5   5                                          I-79        5     5            5   5                                          I-91        5     5            5   5                                          I-92        5     5            5   5                                          I-93        5     5            5   5                                          I-94        5     5            5   5                                          I-95        5     5            5   5                                          I-110       5     5            5   5                                          I-111       5     5            5   5                                          I-112       5     5            5   5                                          I-113       5     5            5   5                                          I-114       5     5            5   5                                          I-120       5     5            5   5                                          I-131       5     5            5   5                                          I-134       5     5            5   5                                          I-136       5     5            5   5                                          I-149       5     5            5   5                                          I-150       5     5            5   5                                          I-151       5     5            5   5                                          I-152       5     5            4   5                                          I-153       5     5            5   5                                          I-157       5     5            5   5                                          I-158       5     5            5   5                                          I-160       5     5            5   5                                          I-161       5     5            5   5                                          I-162       5     5            5   5                                          I-174       5     5            5   5                                          I-175       5     5            5   5                                          I-176       5     5            5   --                                         I-177       5     5            5   --                                         I-178       5     5            5   5                                          I-179       5     5            5   --                                         I-180       5     5            5   5                                          I-181       5     5            5   5                                          I-182       5     5            5   5                                          I-183       5     5            4   5                                          I-184       5     5            4   5                                          I-194       5     5            5   5                                          I-198       5     5            5   5                                          I-199       5     5            5   5                                          I-204       5     5            5   5                                          I-205       5     5            4   5                                          I-209       5     5            4   5                                          I-212       5     5            5   5                                          I-216       5     5            5   5                                          I-218       4     5            4   5                                          I-322       5     5            5   --                                         I-334       5     5            5   --                                         I-337       5     5            5   --                                         I-506       5     5            5   5                                          I-507       5     5            5   5                                          I-508       5     5            5   5                                          I-509       5     5            4   5                                          I-511       5     5            5   4                                          I-513       5     5            5   5                                          I-514       5     5            5   4                                          I-516       5     5            5   5                                          I-517       4     5            4   5                                          I-518       5     5            5   5                                          I-519       5     5            5   5                                          I-520       5     5            5   5                                          I-521       5     5            5   5                                          I-525       5     5            5   5                                          I-526       4     5            4   5                                          I-527       5     5            5   5                                          I-528       5     5            5   5                                          I-529       4     5            5   5                                          I-530       5     5            5   5                                          I-555       5     5            5   5                                          I-641       5     5            5   5                                          I-761       4     5            4   --                                         I-905       5     5            5   --                                         I-906       5     5            5   --                                         II-5        5     5            5   5                                          II-6        5     5            4   5                                          II-8        5     5            5   5                                          II-17       5     5            5   5                                          II-19       5     5            5   5                                          II-20       5     5            5   5                                          II-23       5     5            5   5                                          II-25       5     5            4   5                                          II-26       5     5            5   5                                          II-27       5     5            5   5                                          II-28       5     5            5   5                                          II-29       5     5            5   --                                         II-31       5     5            5   5                                          II-32       5     5            5   5                                          II-34       5     5            5   5                                          II-35       5     5            5   5                                          II-36       5     5            5   5                                          II-38       5     5            4   5                                          II-53       5     5            5   --                                         II-55       5     5            4   5                                          II-56       5     5            5   5                                          II-63       5     5            5   5                                          II-64       5     5            5   5                                          II-65       5     5            5   --                                         II-66       5     5            5   --                                         II-67       5     5            5   --                                         II-90       4     5            5   --                                         II-91       5     5            5   5                                          II-92       5     5            5   5                                          II-93       5     5            4   5                                          II-95       4     5            4   5                                          II-96       5     5            4   5                                          II-104      5     5            5   --                                         II-105      4     5            5   --                                         II-106      5     5            5   5                                          II-107      5     5            5   5                                          II-110      5     5            5   5                                          II-111      5     5            5   5                                          II-113      5     5            5   5                                          II-114      5     5            5   5                                          II-115      5     5            4   4                                          II-120      5     5            5   5                                          II-127      5     5            5   5                                          II-130      5     5            4   5                                          II-131      5     5            5   5                                          II-134      5     5            5   5                                          II-136      5     5            5   5                                          II-137      5     5            5   --                                         II-138      5     5            5   --                                         II-139      5     5            5   --                                         II-140      5     5            4   --                                         II-141      5     5            5   --                                         II-142      5     5            5   --                                         II-143      5     5            5   --                                         II-144      5     5            5   --                                         II-145      5     5            5   --                                         II-146      5     5            5   5                                          II-149      5     5            4   5                                          II-150      5     5            5   5                                          II-155      5     5            5   5                                          II-156      4     5            5   5                                          II-157      5     5            5   5                                          II-158      5     5            5   5                                          II-160      5     5            5   5                                          II-161      4     5            4   5                                          II-162      5     5            5   5                                          II-163      5     5            4   5                                          II-164      5     5            5   5                                          II-166      5     5            5   5                                          II-167      4     5            5   5                                          II-168      5     5            5   5                                          II-169      5     5            5   5                                          II-170      4     5            5   5                                          II-172      5     5            5   5                                          II-174      5     5            5   5                                          II-175      5     5            5   --                                         II-176      5     5            5   --                                         II-177      5     5            5   --                                         II-178      5     5            5   --                                         II-179      5     5            5   --                                         II-180      5     5            5   5                                          II-181      5     5            5   5                                          II-182      5     5            5   5                                          II-183      5     5            4   5                                          II-184      5     5            5   5                                          II-185      5     5            5   --                                         II-188      5     5            5   5                                          II-189      5     5            5   5                                          II-191      5     5            5   --                                         II-195      5     5            5   4                                          II-197      5     5            5   --                                         II-198      5     5            5   --                                         II-199      5     5            5   --                                         II-200      5     5            5   --                                         II-204      5     5            4   5                                          II-207      5     5            4   --                                         II-219      4     5            5   5                                          II-220      5     5            5   --                                         II-223      5     5            5   --                                         II-225      5     5            5   5                                          II-226      5     5            5   5                                          II-227      5     5            5   --                                         II-531      5     5            5   --                                         ______________________________________                                    

TEST EXAMPLE 3 (Test on Herbicidal Effects by Upland Field FoliageTreatment)

In a plastic pot (surface area: 120 cm²) filled with upland field soil,pale smartweed (Po), slender amaranth (Am), common lambsquarters (Ch)and rice flatsedge (Ci) were sown and covered with soil and werecultured in a green house for 2 weeks. A wettable powder prepared inaccordance with Formulation Example 1 was diluted with water and appliedonto the entire foliages of the plants from above by a small-sizedsprayer in an amount of 100 l/10 ares so as to apply 100 g of the activeingredient per 10 ares. The plants were then cultured in the greenhouse, and the evaluation of the herbicidal effects was conducted on the14th day after the treatment in accordance with the standards asidentified in Table 4. The results are shown in Table 7.

                  TABLE 7                                                         ______________________________________                                                    Herbicidal                                                        Compound    effects                                                           No.         Po    Am           Ch  Ci                                         ______________________________________                                        I-5         5     5            5   5                                          I-6         5     5            5   5                                          I-8         5     5            5   5                                          I-17        5     5            5   5                                          I-18        5     5            5   5                                          I-19        5     5            5   5                                          I-20        5     5            5   5                                          I-23        5     5            5   5                                          I-25        5     5            5   5                                          I-26        5     5            5   5                                          I-27        5     5            5   5                                          I-28        5     5            5   5                                          I-29        5     5            5   5                                          I-31        5     5            5   5                                          I-32        5     5            5   5                                          I-33        5     5            5   5                                          I-34        5     5            5   5                                          I-35        5     5            5   5                                          I-53        5     5            5   5                                          I-63        5     5            5   5                                          I-64        5     5            5   5                                          I-65        5     5            5   5                                          I-66        5     5            5   5                                          I-67        5     5            5   5                                          I-79        5     5            5   5                                          I-91        5     5            5   5                                          I-92        5     5            5   5                                          I-93        5     5            5   5                                          I-94        5     5            5   5                                          I-95        5     5            5   5                                          I-111       5     5            5   5                                          I-112       5     5            5   5                                          I-113       5     5            5   5                                          I-114       5     5            5   5                                          I-120       5     5            5   5                                          I-131       5     5            5   5                                          I-134       5     5            5   5                                          I-136       5     5            4   4                                          I-149       4     5            4   5                                          I-150       5     5            5   5                                          I-151       5     5            5   5                                          I-157       5     5            5   5                                          I-158       5     5            5   5                                          I-160       5     5            5   5                                          I-161       5     5            5   5                                          I-162       5     5            5   5                                          I-174       5     5            5   5                                          I-175       5     5            5   5                                          I-176       5     5            5   5                                          I-177       4     4            5   5                                          I-178       5     5            5   5                                          I-179       5     5            5   5                                          I-180       5     5            5   5                                          I-181       5     5            5   5                                          I-182       5     5            5   5                                          I-183       5     5            5   4                                          I-184       5     5            5   5                                          I-194       5     5            5   5                                          I-204       5     5            5   5                                          I-205       5     5            5   5                                          I-206       5     5            5   4                                          I-209       4     5            5   4                                          I-211       4     5            5   4                                          I-212       4     5            5   4                                          I-216       5     5            5   5                                          I-218       5     5            4   4                                          I-322       5     5            5   5                                          I-324       4     5            4   5                                          I-334       5     5            4   5                                          I-337       5     5            5   5                                          I-506       4     5            4   5                                          I-507       5     5            5   5                                          I-508       5     5            5   5                                          I-509       5     5            5   5                                          I-511       4     5            5   4                                          I-513       5     5            5   5                                          I-514       5     5            5   4                                          I-516       5     5            5   5                                          I-517       5     5            4   5                                          I-518       5     5            5   5                                          I-520       5     5            5   5                                          I-525       5     5            5   5                                          I-526       5     5            5   4                                          I-527       5     5            5   5                                          I-528       5     5            5   5                                          I-530       5     5            5   5                                          I-555       5     5            5   5                                          I-641       5     5            5   5                                          II-5        5     5            5   5                                          II-6        4     5            5   5                                          II-8        5     5            4   5                                          II-17       5     5            4   5                                          II-19       5     5            5   5                                          II-20       5     5            5   5                                          II-23       5     5            5   5                                          II-25       5     5            5   5                                          II-26       5     5            5   5                                          II-27       5     5            5   5                                          II-28       5     5            5   5                                          II-29       5     5            5   5                                          II-31       5     5            4   5                                          II-32       5     5            5   5                                          II-34       5     5            5   5                                          II-35       5     5            5   5                                          II-38       5     5            4   5                                          II-53       5     5            5   5                                          II-55       5     5            5   5                                          II-56       5     5            5   5                                          II-63       5     5            5   5                                          II-64       5     5            5   5                                          II-65       5     5            5   5                                          II-66       5     5            5   5                                          II-67       5     5            5   5                                          II-91       5     5            5   5                                          II-92       5     5            5   5                                          II-93       5     5            5   5                                          II-94       5     5            5   5                                          II-104      5     5            5   5                                          II-105      5     5            5   5                                          II-106      5     5            5   5                                          II-107      5     5            5   5                                          II-110      5     5            5   5                                          II-111      5     5            5   5                                          II-112      5     5            5   5                                          II-113      5     5            5   5                                          II-114      5     5            5   5                                          II-115      5     5            4   5                                          II-120      5     5            5   5                                          II-129      5     5            5   5                                          II-130      5     5            5   5                                          II-131      5     5            5   5                                          II-134      5     5            5   5                                          II-136      5     5            4   4                                          II-140      5     5            5   5                                          II-141      4     5            4   5                                          II-142      5     5            5   5                                          II-143      5     5            5   5                                          II-146      5     5            4   5                                          II-149      5     5            5   5                                          II-150      5     5            5   5                                          II-153      5     5            4   4                                          II-154      5     5            5   4                                          II-155      5     5            5   5                                          II-157      5     5            5   5                                          II-158      5     5            4   5                                          II-160      5     5            5   5                                          II-162      5     5            5   5                                          II-166      5     5            5   5                                          II-167      5     5            5   5                                          II-168      5     5            5   5                                          II-169      5     5            5   5                                          II-170      4     5            5   5                                          II-174      5     5            4   5                                          II-175      5     5            4   5                                          II-176      5     4            5   5                                          II-178      5     5            5   5                                          II-179      5     5            5   5                                          II-180      5     5            5   5                                          II-181      5     5            5   5                                          II-182      5     5            5   5                                          II-183      5     5            4   5                                          II-184      5     5            5   5                                          II-188      5     5            5   5                                          II-189      5     5            4   5                                          II-192      4     5            4   5                                          II-194      5     5            5   5                                          II-195      5     5            5   5                                          II-196      4     5            4   5                                          II-197      5     5            5   5                                          II-199      5     5            5   5                                          II-204      5     5            5   5                                          II-218      5     5            5   4                                          II-219      4     5            5   4                                          II-220      5     5            4   5                                          II-225      5     5            5   5                                          II-226      5     5            5   5                                          II-531      5     5            5   5                                          ______________________________________                                    

TEST EXAMPLE 4 (Test on Crop Plant Selectivity by Paddy Field SoilTreatment)

In a 1/10,000a plastic pot, paddy field soil was filled, irrigated,paddled and leveled. Then, barnyardgrass (Ec), monochoria (Mo) andbulrush (Sc) were sown at a depth of 0.5 cm. Further, two seedlings ofrice (Or) of 2 leaf stage was transplanted at a transplantation depth of2 cm. Then, the pot was flooded to a water depth of 3 cm. Next day, aprescribed amount of the active ingredient (g^(ai) /10a) of a wettablepowder prepared in accordance with Formulation Example 1 was dilutedwith water and applied dropwise to the water surface. The plants werethen cultured in a green house, and the evaluation of the herbicidaleffects and phytotoxicity was conducted on the 28th day after theapplication in accordance with the standards as identified in Table 4.The results are shown in Table 8.

                  TABLE 8                                                         ______________________________________                                                             Herbicidal  Phytoto-                                     Compound  Dose       effects     xicity                                       No.       (gai 10a)  Eo    Mo    Sc  Or                                       ______________________________________                                        I-17      25         4     5     5   0                                        I-157     6.3        5     5     5   1                                        I-161     25         5     5     5   0                                        I-174     25         5     5     4   1                                        I-216     25         4     5     4   2                                        II-19     25         5     5     5   0                                                  6.3        5     5     5   0                                        II-23     25         4     5     5   0                                        II-26     25         5     5     5   1                                                  6.3        5     5     5   0                                                  1.6        5     5     4   0                                        II-27     25         5     5     5   0                                                  6.3        5     5     5   0                                        II-29     6.3        5     5     5   1                                                  1.6        3     5     5   0                                        II-31     6.3        5     5     5   1                                                  1.6        5     5     5   0                                        II-35     25         5     5     5   1                                                  6.3        5     5     5   0                                        II-36     25         5     5     5   0                                        II-53     25         5     5     5   0                                        II-64     25         5     5     5   0                                                  6.3        5     5     5   0                                        II-65     25         5     5     5   0                                                  6.3        5     5     5   0                                        II-66     25         5     5     5   1                                                  6.3        S     5     5   0                                        II-92     25         5     5     5   2                                                  6.3        5     5     5   0                                                  1.6        5     5     5   0                                        II-93     25         5     5     5   1                                                  6.3        5     5     5   0                                        II-94     25         5     5     5   1                                                  6.3        5     5     5   0                                        II-104    25         5     5     5   0                                                  6.3        5     5     5   0                                        II-114    6.3        5     5     5   1                                                  1.6        5     5     5   0                                        II-127    25         5     5     5   1                                                  6.3        3     5     5   0                                        II-134    25         5     5     5   0                                                  6.3        5     5     5   0                                        II-137    25         5     5     5   2                                                  6.3        5     5     5   0                                                  1.6        5     5     5   0                                        II-141    25         5     5     5   1                                                  6.3        5     5     4   0                                        II-142    6.3        5     5     5   0                                                  1.6        5     5     5   0                                        II-157    25         5     5     5   0                                                  6.3        5     5     5   0                                        II-160    25         5     5     5   0                                                  6.3        5     5     5   0                                        II-162    25         5     5     5   1                                                  6.3        5     5     5   0                                        II-166    1.6        5     5     5   0                                        II-178    25         5     5     5   0                                                  6.3        4     5     4   0                                        II-208    25         5     5     5   0                                                  6.3        4     5     4   0                                        II-531    25         5     5     5   0                                                  6.3        5     5     4   0                                        Compara-  25         5     5     5   5                                        tive      6.3        5     5     4   5                                        compound  1.6        3     4     2   5                                        ______________________________________                                         Comparative compound A: Disclosed in Japanese Unexamined Patent               Publication No. 95091/1992 (Compound No. 1)                              

TEST EXAMPLE 5 (Test on Crop Plant Selectivity by Upland Field SoilTreatment)

In a plastic pot (surface area: 600 cm²) filled with upland field soil,seeds or tubers of wheat (Tr), corn (Ze), grain sorghum (Gs), palesmartweed (Po), slender amaranth (Am), common lambsquarters (Ch),velvetleaf (Ab), morningglory (Ip), cocklebur (Xa) and purple nutsedge(CR) were planted and covered with soil. Next day, a prescribed amountof the active ingredient (g^(ai) /10a) of a wettable powder prepared inaccordance with Formulation Example 1 was diluted with water and applieduniformly to the soil surface by a small-sized sprayer in an amount of100 l per 10 ares. The plants were then cultured in a green house, andthe evaluation of the herbicidal effects was conducted on the 21st dayafter the application in accordance with the standards as identified inTable 4. The results are shown in Table 9.

                  TABLE 9                                                         ______________________________________                                        Com-            Herbicidal         Phytoto-                                   pound  Dose     effects            xicity                                     No.    (gai 10a)                                                                              Po    Am   Ch  Ab  Ip  Xa  CR  Tr  Ze  Gs                     ______________________________________                                        II-19  25       5     5    5   5   5   5   2   0   1   0                      II-23  25       5     5    5   5   5   5   5   0   3   1                             6.3      4     5    4   5   4   5   5   0   3   0                      II-26  25       5     5    5   5   5   5   --  1   4   3                             6.3      5     5    4   4   4   4   4   0   3   1                      II-28  25       5     5    5   5   5   5   --  0   1   0                             6.3      5     5    4   4   4   4   4   0   0   0                      II-29  25       5     5    5   5   5   5   5   0   3   3                             6.3      5     5    5   5   5   5   5   0   1   1                      II-35  6.3      5     5    5   4   4   4   5   0   1   0                      II-53  25       5     5    5   5   5   5   5   1   2   1                             6.3      5     5    5   5   5   5   4   0   0   0                      II-63  25       5     5    5   5   5   5   5   0   5   3                             6.3      5     5    5   5   5   5   5   0   3   2                      II-64  6.3      5     5    5   5   5   5   5   0   1   3                             1.6      5     5    5   3   5   5   5   0   0   0                      II-65  25       5     5    5   5   5   5   5   1   1   4                             6.3      5     5    5   4   4   5   5   0   0   3                      II-66  25       5     5    5   5   5   5   5   0   4   4                             6.3      5     5    5   5   4   5   5   0   1   3                      II-91  6.3      5     5    5   5   5   5   5   0   4   1                      II-104 25       5     5    5   5   5   5   5   0   4   3                             6.3      5     5    5   4   4   5   5   0   1   3                      II-107 25       5     5    5   5   5   5   5   0   4   4                             6.3      5     5    5   4   3   5   5   0   3   3                      II-134 25       5     5    5   5   5   5   5   1   1   1                             6.3      5     5    5   5   5   5   5   0   0   0                      II-137 25       5     5    5   5   5   5   5   0   4   2                             6.3      5     5    5   5   4   5   5   0   3   1                      II-142 25       5     5    5   5   5   5   5   1   4   4                             6.3      5     5    5   5   5   5   5   0   3   3                      II-157 25       5     5    5   5   5   5   4   2   4   0                             6.3      5     5    5   5   3   5   3   0   1   0                      II-168 25       5     5    5   5   5   5   4   1   4   4                             6.3      5     5    5   4   4   5   3   0   3   3                      II-215 25       5     5    5   4   5   5   5   1   2   1                      ______________________________________                                    

TEST EXAMPLE 5 (Test on Crop Plant Selectivity by Upland Field FoliageTreatment)

In a plastic pot (surface area: 600 cm²) filled with upland field soil,seeds or tubers of wheat (Tr), corn (Ze), grain sorghum (Gs), palesmartweed (Po), slender amaranth (Am), common lambsquarters (Ch),velvetleaf (Ab), morningglory (Ip), cocklebur (Xa) and purple nutsedge(CR) were planted, covered with soil and cultured in a green house for 2weeks. Then, a prescribed amount of the active ingredient (g^(ai) /10a)of a wettable powder prepared in accordance with Formulation Example 1was diluted with water and applied onto the entire foliages of theplants from above by a small-sized sprayer in an amount of 100 l per 10ares. The plants were then cultured in a green house, and the evaluationof the herbicidal effects was conducted on the 14th day after thetreatment in accordance with the standards as identified in Table 4. Theresults are shown in Table 10.

                  TABLE 10                                                        ______________________________________                                        Com-       Herbicidal         Phytotox-                                       pound Dose     effects            icity                                       No.   (gai 10 a)                                                                             Po    Am   Ch  Ab  Ip  Xa  CR  Tr   Ze  Gs                     ______________________________________                                        I-20  6.3      5     5    5   5   5   5   3   1    3   3                      I-23  25       5     5    5   5   5   5   2   0    4   3                            6.3      5     5    5   5   5   5   0   0    3   3                      I-26  1.6      5     5    5   5   5   5   5   1    4   4                      I-27  6.3      5     5    5   5   5   5   3   1    3   3                            1.6      5     5    4   5   5   5   1   0    3   3                      I-28  25       5     5    5   5   5   5   2   1    3   3                            6.3      5     5    4   5   4   5   1   0    3   3                      I-53  25       5     5    5   5   5   5   3   1    3   3                            6.3      5     5    5   5   5   5   1   0    3   2                      I-66  6.3      5     5    5   5   5   5   2   1    3   --                     I-176 25       5     5    5   5   5   5   3   1    3   3                            6.3      5     5    5   5   5   4   2   0    3   3                      I-194 25       5     5    4   5   5   5   3   0    4   4                      I-204 25       5     5    4   5   5   5   --  1    4   4                            6.3      4     5    4   5   5   5   --  0    4   3                      I-337 25       5     5    5   5   5   5   4   1    4   3                            6.3      4     5    5   5   5   5   4   0    3   3                      I-516 25       4     5    5   5   5   5   2   0    4   3                      II-20 25       5     5    5   5   5   5   5   0    4   3                            6.3      5     5    5   5   5   5   5   0    4   3                      II-26 25       5     5    5   5   5   5   5   0    3   1                            6.3      5     5    5   5   5   5   5   0    2   1                      II-27 25       5     5    5   5   5   5   2   0    0   0                            6.3      5     5    5   5   5   5   1   0    0   0                      II-28 25       5     5    5   5   5   5   --  1    3   3                            6.3      5     5    5   5   5   5   5   0    2   2                      II-31 25       5     5    5   5   5   5   5   1    1   1                            6.3      5     5    4   5   5   5   5   0    1   1                      II-64 25       5     5    5   5   5   5   4   0    0   3                            6.3      5     5    5   5   5   5   4   0    0   2                      II-93 25       5     5    5   5   5   5   5   1    1   3                            6.3      5     5    5   5   5   5   5   0    1   3                      II-104                                                                              100      5     5    5   5   5   5   5   0    0   3                            25       5     5    5   5   5   5   4   0    0   3                      II-127                                                                              25       5     5    4   5   5   5   5   0    4   1                      II-134                                                                              25       5     5    5   5   5   5   5   0    0   0                            6.3      5     5    4   5   5   5   5   0    0   0                      II-150                                                                              25       5     5    4   5   5   5   --  0    1   3                      II-157                                                                              25       5     5    5   5   5   5   --  0    0   2                            6.3      5     5    4   5   5   5   --  0    0   1                      II-168                                                                              25       5     5    5   5   5   5   4   1    4   3                            6.3      5     5    4   5   5   5   3   0    2   3                      II-180                                                                              25       5     5    5   5   5   5   --  0    0   1                            6.3      5     5    4   5   5   5   --  0    0   1                      II-181                                                                              25       5     5    5   5   5   5   5   1    3   2                            6.3      5     5    5   5   5   5   4   0    1   1                      ______________________________________                                    

We claim:
 1. An indazolesulfonamide derivative represented by theformula: ##STR79## wherein R¹ is a hydrogen atom, a C₁₋₃₀ -alkyl group,a C₃₋₇ -cycloalkyl group, a halo-C₁₋₃₀ -alkyl group, a C₁₋₃₀-alkoxy-C₁₋₃₀ -alkyl group, a benzyloxy-C₁₋₃₀ -alkyl group, a benzylgroup, a phenyl group, a pyridyl group, a di-C₁₋₃₀ -alkylaminocarbonylgroup, a C₁₋₃₀ -alkoxycarbonyl group, a C₁₋₃₀ -alkylsulfonyl group, aphenylsulfonyl group, a di-C₁₋₃₀ -alkylaminosulfonyl group, a halo-C₁₋₃₀-alkylcarbonyl group, a C₁₋₃₀ -alkylcarbonyl group, a benzoyl group or aC₂₋₂₀ -alkenyl group, R² and R³ are the same or different and representa hydrogen atom, a halogen atom, a C₁₋₃₀ -alkyl group, a C₃₋₇-cycloalkyl group, a C₂₋₂₀ -alkenyl group, a C₁₋₃₀ -alkoxycarbonyl-C₂₋₂₀-alkenyl group, a C₂₋₂₀ -alkynyl group, a halo-C₁₋₃₀ -alkyl group, aC₁₋₃₀ -alkoxy-C₁₋₃₀ -alkyl group, a C₁₋₃₀ -alkoxycarbonyl-C₁₋₃₀ -alkylgroup, a C₁₋₃₀ -alkylcarbonyl-C₁₋₃₀ -alkyl group, a C₃₋₇-cycloalkylcarbonyl-C₁₋₃₀ -alkyl group, a cyano-C₁₋₃₀ -alkyl group, adi-C₁₋₃₀ -alkylaminocarbonyl-C₁₋₃₀ -alkyl group, a di-C₁₋₃₀-alkylamino-C₁₋₃₀ -alkyl group, a di-C₁₋₃₀ -alkylaminosulfonyl-C₁₋₃₀-alkyl group, an azido-C₁₋₃₀ -alkyl group, a benzyl group, a phenylgroup, a nitro group, a cyano group, an azide group, an amino group, amono C₁₋₃₀ -alkylamino group, a di-C₁₋₃₀ -alkylamino group, abenzylamino group, a C₁₋₃₀ -alkylcarbonylamino group which optionally issubstituted by a halogen atom, a benzoylamino group, a C₁₋₃₀-alkoxycarbonylamino group, a phenoxycarbonylamino group, a C₁₋₃₀-alkylsulfonylamino group wherein the amino group optionally issubstituted by a C₁₋₃₀ -alkyl group, a phenylsulfonylamino group whereinthe amino group optionally is substituted by a C₁₋₃₀ -alkyl group, aC₁₋₃₀ -alkylideneamino group, a benzylideneamino group, a tetrazolylgroup which optionally is substituted by a methyl group, a grouprepresented by the formula --COR⁴ wherein R⁴ is a hydrogen atom, ahydroxyl group, a C₁₋₃₀ -alkyl group, a C₃₋₇ -cycloalkyl group, ahalo-C₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenyl group, a C₂₋₂₀ -alkynyl group,a benzyl group, a phenyl group, a C₁₋₃₀ -alkoxy group, a halo-C₁₋₃₀-alkoxy group, a C₁₋₃₀ -alkoxy-C₁₋₃₀ - alkoxy group, a C₂₋₂₀ -alkenyloxygroup, a halo-C₂₋₂₀ -alkenyloxy group, a C₂₋₂₀ -alkynyloxy group, abenzyloxy group or a phenoxy group; a group represented by the formula--C(O)NR⁵ R⁶ wherein R⁵ and R⁶ are the same or different and represent ahydrogen atom, a C₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenyl group, a C₂₋₂₀-alkynyl group, a benzyl group, a phenyl group or a C₁₋₃₀ -alkoxy group;a group represented by the formula --SR⁷ wherein R⁷ is a hydrogen atom,a C₁₋₃₀ -alkyl group or a halo-C₁₋₃₀ -alkyl group; a group representedby the formula --So₂ NR⁵ R⁶, wherein R⁵ and R⁶ have the same meanings asdefined above; a group represented by the formula --S(O)_(n) R⁸, whereinn represents an integer of 1 or 2, and R⁸ represents a C₁₋₃₀ -alkylgroup, a C₂₋₂₀ -alkenyl group or a halo-C₁₋₃₀ -alkyl group; a grouprepresented by the formula --OR⁹, wherein R⁹ is a hydrogen atom, a C₁₋₃₀-alkyl group, a C₃₋₇ -cycloalkyl C₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenylgroup, a C₂₋₂₀ -alkynyl group, a benzyl group optionally substituted bya halogen atom, a C₁₋₃₀ -alkyl group or a C₁₋₃₀ -alkoxy group; ahalo-C₁₋₃₀ -alkyl group, a halo-C₂₋₂₀ -alkenyl group, a phenyl groupoptionally substituted by a halogen atom, a C₁₋₃₀ -alkyl group or aC₁₋₃₀ -alkoxy group; a C₁₋₃₀ -alkoxy-C₁₋₃₀ -alkyl group, a C₁₋₃₀-alkoxy-C₁₋₃₀ -alkoxy-C₁₋₃₀ -alkyl group, a halo-C₁₋₃₀ -alkoxy-C₁₋₃₀-alkyl group, a benzyloxy-C₁₋₃₀ -alkyl group, a phenoxy-C₁₋₃₀ -alkylgroup, a C₁₋₃₀ -alkylthio-C₁₋₃₀ -alkyl group, a di-C₁₋₃₀-alkylamino-C₁₋₃₀ -alkyl group, an azido C₁₋₃₀ -alkyl group, a C₁₋₃₀-alkylcarbonyl group, a halo-C₁₋₃₀ -alkylcarbonyl group, a benzoylgroup, a di-C₁₋₃₀ -alkylaminocarbonyl group, a cyano-C₁₋₃₀ -alkyl group,a C₁₋₃₀ -alkylideneamino group, a di-C₁₋₃₀ -alkylideneamino group, abenzylideneamino group or a C₁₋₃₀ -alkoxycarbonyl-C₁₋₃₀ -alkyl group; orthe formula --C(═NOR¹⁰)R¹¹, wherein R¹⁰ represents a hydrogen atom, aC₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenyl group, a C₂₋₂₀ -alkynyl group, abenzyl group, a halo-C₁₋₃₀ -alkyl group or a phenyl group, and R¹¹represents a hydrogen atom, a C₁₋₃₀ -alkyl group, a benzyl group, ahalo-C₁₋₃₀ -alkyl group or a phenyl group, and R² and R³ together mayform a --OC₂ H₄ O--, --SC₂ H₄ S-- or --OCH₂ -- group.
 2. Anindazolesulfonamide derivative represented by the formula: ##STR80##wherein R¹ is a hydrogen atom, a C₁₋₃₀ -alkyl group, a C₃₋₇ -cycloalkylgroup, a halo-C₁₋₃₀ -alkyl group, a C₁₋₃₀ -alkoxy-C₁₋₃₀ -alkyl group, abenzyloxy-C₁₋₃₀ -alkyl group, a benzyl group, a phenyl group, a pyridylgroup, a di-C₁₋₃₀ -alkylaminocarbonyl group, a C₁₋₃₀ -alkoxycarbonylgroup, a C₁₋₃₀ -alkylsulfonyl group, a phenylsulfonyl group, a di-C₁₋₃₀-alkylaminosulfonyl group, a halo-C₁₋₃₀ -alkylcarbonyl group, a C₁₋₃₀-alkylcarbonyl group, a benzoyl group or a C₂₋₂₀ -alkenyl group, R² andR³ are the same or different and represent a hydrogen atom, a halogenatom, a C₁₋₃₀ -alkyl group, a C₃₋₇ -cycloalkyl group, a C₂₋₂₀ -alkenylgroup, a C₁₋₃₀ -alkoxycarbonyl-C₂₋₂₀ -alkenyl group, a C₂₋₂₀ -alkynylgroup, a halo-C₁₋₃₀ -alkyl group, a C₁₋₃₀ -alkoxy-C₁₋₃₀ -alkyl group, aC₁₋₃₀ - alkoxycarbonyl-C₁₋₃₀ -alkyl group, a C₁₋₃₀ -alkylcarbonyl-C₁₋₃₀-alkyl group, a C₃₋₇ -cycloalkylcarbonyl-C₁₋₃₀ -alkyl group, acyano-C₁₋₃₀ -alkyl group, a di-C₁₋₃₀ -alkylaminocarbonyl-C₁₋₃₀ -alkylgroup, a di-C₁₋₃₀ alkylamino-C₁₋₃₀ -alkyl group, a di-C₁₋₃₀-alkylaminosulfonyl-C₁₋₃₀ -alkyl group, an azido-C₁₋₃₀ -alkyl group, abenzyl group, a phenyl group, a nitro group, a cyano group, an azidegroup, an amino group, a mono-C₁₋₃₀ -alkylamino group, a di-C₁₋₃₀-alkylamino group, a benzylamino group, a C₁₋₃₀ -alkylcarbonylaminogroup which optionally is substituted by a halogen atom, a benzoylaminogroup, a C₁₋₃₀ -alkoxycarbonylamino group, a phenoxycarbonylamino group,a C₁₋₃₀ -alkylsulfonylamino group wherein the amino group optionally issubstituted by a C₁₋₃₀ -alkyl group, a phenylsulfonylamino group whereinthe amino group optionally is substituted by a C₁₋₃₀ -alkyl group, aC₁₋₃₀ -alkylideneamino group, a benzylideneamino group, a tetrazolylgroup which optionally is substituted by a methyl group, a grouprepresented by the formula --COR⁴, wherein R⁴ is a hydrogen atom, ahydroxyl group, a C₁₋₃₀ -alkyl group, a C₃₋₇ -cycloalkyl group, ahalo-C₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenyl group, a C₂₋₂₀ -alkynyl group,a benzyl group, a phenyl group, a C₁₋₃₀ -alkoxy group, a halo-C₁₋₃₀-alkoxy group, a C₁₋₃₀ -alkoxy-C₁₋₃₀ - alkoxy group, a C₂₋₂₀ -alkenyloxygroup, a halo-C₂₋₂₀ -alkenyloxy group, a C₂₋₂₀ -alkynyloxy group, abenzyloxy group or a phenyloxy group; a group represented by the formula--C(O)NR⁵ R⁶, wherein R⁵ and R⁶ are the same or different and representa hydrogen atom, a C₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenyl group, a C₂₋₂₀ -alkynyl group, a benzyl group, a phenyl group or a C₁₋₃₀ -alkoxy group;a group represented by the formula --SR⁷, wherein R⁷ is a hydrogen atom,a C₁₋₃₀ -alkyl group or a halo-C₁₋₃₀ -alkyl group; a group representedby the formula --SO₂ NR⁵ R⁶, wherein R⁵ and R⁶ have the same meanings asdefined above; a group represented by the formula --S(O)_(n) R⁸, whereinn represents an integer of 1 or 2, and R⁸ represents a C₁₋₃₀ -alkylgroup, a C₂₋₂₀ -alkenyl group or a halo-C₁₋₃₀ -alkyl group; a grouprepresented by the formula --OR⁹, wherein R⁹ is a hydrogen atom, a C₁₋₃₀-alkyl group, a C₃₋₇ -cycloalkyl-C₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenylgroup, a C₂₋₂₀ - alkynyl group, a benzyl group optionally substituted bya halogen atom, a C₁₋₃₀ -alkyl group or a C₁₋₃₀ -alkoxy group; ahalo-C₁₋₃₀ -alkyl group, a halo-C₂₋₂₀ -alkenyl group, a phenyl groupoptionally substituted by a halogen atom, a C₁₋₃₀ -alkyl group or aC₁₋₃₀ -alkoxy group; a C₁₋₃₀ -alkoxy-C₁₋₃₀ -alkyl group, a C₁₋₃₀-alkoxy-C₁₋₃₀ -alkoxy-C₁₋₃₀ -alkyl group, a halo-C₁₋₃₀ -alkoxy-C₁₋₃₀-alkyl group, a benzyloxy-C₁₋₃₀ -alkyl group, a phenoxy-C₁₋₃₀ - alkylgroup, a C₁₋₃₀ -alkylthio-C₁₋₃₀ -alkyl group, a di-C₁₋₃₀-alkylamino-C₁₋₃₀ -alkyl group, an azido-C₁₋₃₀ -alkyl group, a C₁₋₃₀-alkylcarbonyl group, a halo-C₁₋₃₀ -alkylcarbonyl group, a benzoylgroup, a di-C₁₋₃₀ -alkylaminocarbonyl group, a cyano-C₁₋₃₀ -alkyl group,a C₁₋₃₀ -alkylideneamino group, a di-C₁₋₃₀ -alkylideneamino group, abenzylideneamino group or a C₁₋₃₀ -alkoxycarbonyl-C₁₋₃₀ -alkyl group, orthe formula --C(═NOR¹⁰)R¹¹, wherein R¹⁰ represents a hydrogen atom, aC₁₋₃₀ -alkyl group, a C₂₋₂₀ -alkenyl group, a C₂₋₂₀ -alkynyl group, abenzyl group, a halo-C₁₋₃₀ -alkyl group or a phenyl group, and R¹¹represents a hydrogen atom, a C₁₋₃₀ -alkyl group, a benzyl group, ahalo-C₁₋₃₀ -alkyl group or a phenyl group, and R² and R³ together mayform a --OC₂ H₄ O--, --SC₂ H₄ S-- or --OCH₂ O-- group.